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696 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27876250 60 Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI Jagiellonian University Medical College
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27676089 35 A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-AffinityÁ Opioid Receptor Antagonists.EBI Clinical Research Institute of Montreal
27567368 12 Structural determinants of diphenethylamines for interaction with the┐ opioid receptor: Synthesis, pharmacology and molecular modeling studies.EBI University of Innsbruck
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
27301366 30 [Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.EBI Nanjing Medical University
27148755 75 Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-EfficacyÁ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands.EBI University of Michigan
27190594 2 Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans.EBI Ironwood Pharmaceuticals, Inc.
27185012 8 Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral┐-opioid receptor agonists.EBI China Pharmaceutical University
27096047 73 Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.EBI Fudan University
27035422 46 Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.EBI Vrije Universiteit Brussel
27234885 31 Evaluation of N-substituent structural variations in opioid receptor profile of LP1.EBI University of Catania
27079125 56 Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.EBI Kitasato University
26988801 55 Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI Jagiellonian University Medical College
26390077 42 Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI University of Minnesota
26713104 24 Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.EBI University of Michigan
26944625 26 Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.EBI Medical University of Lodz
26785295 35 Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.EBI Medical University of Lodz
26656913 85 Multitarget opioid ligands in pain relief: New players in an old game.EBI University of Catania
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26789491 44 PotentÁ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.EBI Torrey Pines Institute for Molecular Studies
26524472 75 Further Optimization and Evaluation of Bioavailable, Mixed-EfficacyÁ-Opioid Receptor (MOR) Agonists/d-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.EBI University of Michigan
26491810 35 Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.EBI The University of Kansas
26411794 46 Conformationally restricted┐-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.EBI Mercachem
26330078 51 Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective┐-opioid receptor agonists.EBI Harvard Medical School
26346669 53 Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.EBI University of Tsukuba
26252963 15 Novel diazabicycloalkane delta opioid agonists.EBI Istituto di Farmacologia Traslazionale
26125201 62 Structural Requirements for CNS Active Opioid Glycopeptides.EBI The University of Arizona
26048798 45 Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.EBI Kitasato University
25283554 43 Design, synthesis, and structure-activity relationship of novel opioid┐ receptor selective agonists:a-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.EBI Kitasato University
25168746 28 Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin.EBI University of Monastir
25147605 52 Synthesis and Pharmacology of a Novel┐ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.EBI Kitasato University
25147603 39 Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.EBI Pharmacokinetics
25147602 43 Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.EBI Pharmacokinetics
25129170 20 'Carba'-carfentanil (trans isomer): aÁ opioid receptor (MOR) partial agonist with a distinct binding mode.EBI Clinical Research Institute of Montreal
25593096 65 Potency enhancement of the┐-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.EBI University of Kansas Specialized Chemistry Center
25996309 49 Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities atÁ (MOR),d (DOR), and┐ (KOR) Opioid Receptors.EBI Torrey Pines Institute for Molecular Studies
26005537 72 Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.EBI Medical University of Lodz
25898137 61 C7▀-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.EBI University of Bath
25599950 79 Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.EBI National Institute on Drug Abuse
25559207 92 Synthesis and biological evaluations of novel endomorphin analogues containinga-hydroxy-▀-phenylalanine (AHPBA) displaying mixedÁ/d opioid receptor agonist andd opioid receptor antagonist activities.EBI Zhejiang University
25783191 87 Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14▀-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.EBI Virginia Commonwealth University
25513968 21 Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.EBI Universit£ de Caen Basse-Normandie
25599839 75 Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.EBI Dr. Reddy's Laboratories Ltd
25556095 32 A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.EBI West Chester University
25133923 13 Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.EBI Research Triangle Institute
25087049 56 Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.EBI National Health Research Institutes
25062506 102 Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted┐-opioid receptor agonists.EBI Westf£lische Wilhelms-Universit£t M£nster
25047937 9 Antinociceptive and antidepressant-like action of endomorphin-2 analogs with proline surrogates in position 2.EBI Medical University of Lodz
24973818 70 Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.EBI University of Bath
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
25456075 16 Cyclic side-chain-linked opioid analogs utilizing cis- and trans-4-aminocyclohexyl-D-alanine.EBI TBA
25426797 48 Synthesis and┐-opioid receptor activity of furan-substituted salvinorin A analogues.EBI The University of Kansas
25268943 116 Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.EBI The University of Mississippi
25248680 67 Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.EBI Kitasato University
25221662 24 Novel cyclic biphalin analogue with improved antinociceptive properties.EBI Universit£ di Chieti-Pescara"G. d'Annunzio"
25193297 91 Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.EBI University of Mississippi
24856182 23 Combination of cyclohexane and piperazine based┐-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.EBI Institut f£r Pharmazeutische und Medizinische Chemie der Universit£t M£nster
24933507 15 Synthesis and evaluation of three structurally related╣8F-labeled orvinols of different intrinsic activities: 6-O-[╣8F]fluoroethyl-diprenorphine ([╣8F]FDPN), 6-O-[╣8F]fluoroethyl-buprenorphine ([╣8F]FBPN), and 6-O-[╣8F]fluoroethyl-phenethyl-orvinol ([╣8F]FPEO).EBI University of Oslo
24835200 18 Design and synthesis of quinolinopropellane derivatives with selectived opioid receptor agonism.EBI University of Tsukuba
24761755 76 Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.EBI University of Bath
24690494 92 Antagonists of the kappa opioid receptor.EBI The Scripps Research Institute
24657054 66 Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.EBI Astraea Therapeutics, LLC.
24613457 64 Endomorphin analogues with mixedÁ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lacking▀-arrestin2 recruitment activity.EBI Nanjing Medical University
24602401 40 [Dmt(1)]DALDA analogues with enhancedÁ opioid agonist potency and with a mixedÁ/┐ opioid activity profile.EBI Nanjing Medical University
24678969 44 Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.EBI Centro de Investigaci�n Lilly
24641190 16 Development of a bioavailableÁ opioid receptor (MOPr) agonist,d opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.EBI University of Michigan
15743203 272 3D-QSAR comparative molecular field analysis on opioid receptor antagonists: pooling data from different studies.EBI University of Medicine& Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS)
23434225 37 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors.EBI Rensselaer Polytechnic Institute
23477419 64 Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.EBI Lanzhou University
23438330 174 Orvinols with mixed kappa/mu opioid receptor agonist activity.EBI University of Bath
23419026 40 Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands.EBI University of Michigan
23360448 18 Development of¿ opioid receptor antagonists.EBI Research Triangle Institute
23200250 36 The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.EBI Kitasato University
16290934 51 Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.EBI Pfizer Global Research and Development
22541041 84 Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.EBI Centro de Investigaci�n Lilly
19527931 19 Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide.EBI University of Ferrara
21193310 81 Tetrahydroquinoline derivatives as opioid receptor antagonists.EBI GlaxoSmithKline
19473027 21 Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.EBI National Institute of Neuroscienc
23142613 101 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: oxygenated N-(2-[1,1'-biphenyl]-4-ylethyl) analogues of 8-CAC.EBI Rensselaer Polytechnic Institute
23131341 50 Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).EBI Kitasato University
23116891 15 Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.EBI Kitasato University
23103094 39 Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 3: synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies.EBI Kitasato University
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI The University of Sydney
22325949 28 Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at thed opioid receptor. Discovery of two highly potent and selectived opioid agonists.EBI Clinical Research Institute of Montreal
23134120 72 Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.EBI University of Innsbruck
23116124 65 Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selectiveµ opioid receptor Agents.EBI Virginia Commonwealth University
23102273 60 Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.EBI Vrije Universiteit Brussel
23043264 20 Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversibleµ opioid receptor antagonist effects.EBI University of Bristol
23016952 71 14-Alkoxy- and 14-acyloxypyridomorphinans:µ agonist/d antagonist opioid analgesics with diminished tolerance and dependence side effects.EBI Southern Research Institute
22995061 37 Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.EBI University of Bologna
22966938 20 cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.EBI Universit£ di Chieti-Pescara G. d'Annunzio
22734622 78 Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associatedµ opioid receptor (MOR-1) splice variants.EBI Memorial Sloan-Kettering Cancer Center
23017884 4 Formylated polyamines as peptidomimetics.EBI The Scripps Research Institute
22695132 56 Identification of a duald OR antagonist/µ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).EBI Janssen Research and Development, L.L.C.
22680612 11 Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.EBI The University of Queensland
21978284 42 Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.EBI Vrije Universiteit Brussel
22967810 102 Synthesis of quinolinomorphinan derivatives as highly selectived opioid receptor ligands.EBI Kitasato University
22742909 24 Essential structure of opioid¿ receptor agonist nalfurafine for binding to the¿ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.EBI Kitasato University
22677527 38 Deconstructing 14-phenylpropyloxymetopon: minimal requirements for binding to mu opioid receptors.EBI University of Maryland
22439881 157 Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.EBI Harvard Medical School
22583618 8 Kappa agonist CovX-Bodies.EBI Pfizer Inc.
22464684 85 Semisynthetic neoclerodanes as kappa opioid receptor probes.EBI The University of Kansas
22460026 39 Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.EBI Kitasato University
22445285 26 Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.EBI Kitasato University
21641798 16 Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.EBI Kitasato University
21621410 44 Generation of novel radiolabeled opiates through site-selective iodination.EBI Memorial Sloan-Kettering Cancer Center
21428406 70 N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.EBI National Institute of Mental Health
21351746 116 Aminothiazolomorphinans with mixed¿ andµ opioid activity.EBI Harvard Medical School
21207959 69 Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI National Institute of Mental Health
21216504 19 Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.EBI University of Cagliari
20875743 90 Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relaEBI Pfizer Inc.
20931963 112 Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.EBI ASKA Pharmaceutical Co, Ltd
20727749 17 Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).EBI University of Sydney
20599386 46 Evaluation of N-substitution in 6,7-benzomorphan compounds.EBI University of Catania
20580236 60 Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.EBI University of Innsbruck and Center for Molecular Biosciences Innsbruck-CMBI
20684563 176 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI H. Lundbeck A/S
20478711 12 Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.EBI Kitasato University
20568781 32 Analogues of (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in vitro and in vivo opioid receptor antagonist activity.EBI Research Triangle Institute
20441176 76 Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.EBI Wilhelms-Universit£t M£nster
20218625 27 "Carba"-analogues of fentanyl are opioid receptor agonists.EBI Clinical Research Institute of Montreal
19963380 38 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI Hunter College and the Graduate Center of the City University of New York
19962305 2 Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.EBI Kitasato University
19683449 116 Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.EBI Human BioMolecular Research Institute
19595591 37 Synthesis and opioid receptor activity of indolopropellanes.EBI Chinese Academy of Sciences
19362480 22 Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.EBI Kitasato University
19349178 4 Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.EBI Kitasato University
19464172 74 Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.EBI Adolor Corporation
19282177 106 Syntheses of novel high affinity ligands for opioid receptors.EBI Rensselaer Polytechnic Institute
19217280 34 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.EBI Virginia Commonwealth University
19211245 27 Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.EBI Harvard Medical School
18403056 8 Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?EBI Universit£t des Saarlandes
19253983 37 14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.EBI University of Bath
18755589 2 Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.EBI Kitasato University
19125610 82 Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.EBI Pfizer Inc.
19199782 72 Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.EBI Virginia Commonwealth University
18788723 61 Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).EBI Adolor Corporation
19027293 149 Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.EBI Rensselaer Polytechnic Institute
18990576 11 Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology.EBI Kitasato University
18829333 28 Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.EBI Toray Industries, Inc.
18637671 21 Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.EBI Toray Industries, Inc
17702750 1 Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.EBI University of Washington
18468907 64 Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.EBI Torrey Pines Institute for Molecular Studies
18468904 48 High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI Purdue University
18417347 62 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.EBI Rensselaer Polytechnic Institute
18337104 7 Syntheses of 4,6'-epoxymorphinan derivatives and their pharmacologies.EBI Kitasato University
18502123 68 Development of potent and selective small-molecule human Urotensin-II antagonists.EBI GlaxoSmithKline Pharmaceuticals
18487043 64 Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.EBI Adolor Corporation
18380425 90 Herkinorin analogues with differential beta-arrestin-2 interactions.EBI The University of Iowa
18249546 11 Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.EBI Westf£lische Wilhelms-Universit£t
18166466 12 Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.EBI Harvard Medical School
17981041 79 Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.EBI McLean Hospital
18468891 59 Identification of novel benzimidazole series of potent and selective ORL1 antagonists.EBI Banyu Tsukuba Research Institute
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18293909 5 Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.EBI University of Minnesota
17935988 82 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.EBI Institute
17659872 15 3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.EBI University of Maryland
17980586 79 Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.EBI Lilly Research Laboratories
17887741 133 Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.EBI University of Bath
17420073 31 Synthesis of bridged piperazines with sigma receptor affinity.EBI Institut f£r Pharmazeutische und Medizinische Chemie
17580847 67 Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.EBI The University of Iowa
17428659 192 Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.EBI Schering-Plough Research Institute
17276685 70 High-affinity carbamate analogues of morphinan at opioid receptors.EBI Harvard Medical School
17407276 45 Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.EBI Harvard Medical School
17402725 9 Indium-labeled macrocyclic conjugates of naltrindole: high-affinity radioligands for in vivo studies of peripheral delta opioid receptors.EBI University of Missouri-Columbia
15588100 68 Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.EBI University of Bath
17149858 53 Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.EBI Adolor Corporation
17149859 215 Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.EBI Adolor Corporation
17004724 146 Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.EBI University of Bristol
16942039 54 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.EBI Rensselaer Polytechnic Institute
16913723 78 Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.EBI University of Bristol
16777416 80 Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners.EBI University of Kentucky
16821764 54 Discovery of novel triazole-based opioid receptor antagonists.EBI University of Medicine and Dentistry of New Jersey and UMDNJ Informatics Institute
16650985 1 A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.EBI KAIST
16392810 100 Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.EBI Harvard Medical School
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes for BioMedical Research
15857143 48 Synthesis and biological evaluation of 14-alkoxymorphinans. 22.(1) Influence of the 14-alkoxy group and the substitution in position 5 in 14-alkoxymorphinan-6-ones on in vitro and in vivo activities.EBI University La Sapienza
16033285 24 Effect of a 6-cyano substituent in 14-oxygenated N-methylmorphinans on opioid receptor binding and antinociceptive potency.EBI University of Innsbruck
15456250 54 Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.EBI University of Bath
15808478 18 Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.EBI Rensselaer Polytechnic Institute
15993589 22 Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.EBI Harvard Medical School
15869877 37 Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).EBI McLean Hospital
15380196 141 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.EBI Purdue Pharma LP
15055988 49 2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.EBI Harvard Medical School
14998329 142 Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].EBI Southern Research Institute
14761209 15 Importance of phenolic address groups in opioid kappa receptor selective antagonists.EBI Research Triangle Institute
15239663 60 Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.EBI Abbott Laboratories
12699394 30 Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.EBI University of Innsbruck
12672258 99 14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.EBI University of Bath
12593647 49 2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.EBI Harvard University
14640558 54 Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.EBI University of Bath
14613319 93 Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.EBI Harvard Medical School
12519069 60 The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.EBI University of Bath
12954070 24 Synthesis and biological evaluation of 14-alkoxymorphinans. 20. 14-phenylpropoxymetopon: an extremely powerful analgesic.EBI University of Innsbruck
12930147 96 Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.EBI Universit£ degli Studi di Siena
12825957 60 Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.EBI University of Bath
12825951 54 Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.EBI Research Triangle Institute
12801235 5 Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.EBI University of Vermont
12747782 79 Structure-activity relationships of dynorphin a analogues modified in the address sequence.EBI University of California
12723940 145 2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.EBI Research Triangle Institute
12502358 126 The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.EBI Universit£ de Montr£al
11906279 2 Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.EBI TBA
12431065 72 Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.EBI University of Innsbruck
12431062 33 Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.EBI Universit£ de Montr£al
11784158 28 4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.EBI University of Bristol
12139463 24 Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.EBI Research Triangle Institute
11311071 53 Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.EBI National Institute of Diabetes and Digestive and Kidney Diseases
11297446 3 Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).EBI University of Minnesota
11300879 77 Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.EBI Research Triangle Institute
11300867 32 Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the"address" recognition locus.EBI University of Minnesota
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI F-59000 Lille
11585443 137 From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.EBI F-59000 Lille
11543672 24 [2',6'-Dimethyltyrosine]dynorphin A(1-11)-NH2 analogues lacking an N-terminal amino group: potent and selective kappa opioid antagonists.EBI Clinical Research Institute of Montreal
11495592 12 Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.EBI Pharmazeutisches Institut der Universit£t Freiburg
11495579 24 Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.EBI Research Triangle Institute
11405645 13 Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.EBI University of Minnesota
10794701 48 Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.EBI University of Bristol
10780914 37 Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.EBI University of Minnesota
10753470 95 High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.EBI F. Hoffmann-La Roche Ltd.
10753461 13 Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.EBI University of Minnesota
10669565 20 Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.EBI University of Minnesota
10649968 28 Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.EBI University of Bristol
11000010 27 Selective protection and functionalization of morphine: synthesis and opioid receptor binding properties of 3-amino-3-desoxymorphine derivatives.EBI Rensselaer Polytechnic Institute
10966754 9 3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.EBI University of Bristol
10956208 121 Nonpeptide analogues of dynorphin A(1-8): design, synthesis, and pharmacological evaluation of kappa-selective agonists.EBI University of Catania
10893307 26 [Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.EBI University of California
10891107 3 Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.EBI University of Minnesota
10841791 8 Modeling of kappa-opioid receptor/agonists interactions using pharmacophore-based and docking simulations.EBI Universit£ di Napoli"Federico II"
10633042 30 Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.EBI Harvard Medical School
10229636 30 delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.EBI National Institute of Diabetes
10639287 62 Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.EBI National Institute of Diabetes and Digestive and Kidney Diseases
10508425 68 Mixture-based synthetic combinatorial libraries.EBI Torrey Pines Institute for Molecular Studies
10479286 53 Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.EBI Southern Research Institute
9857089 32 Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.EBI Research Triangle Institute
9857087 63 Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.EBI Vrije Universiteit Brussel
9836606 12 Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.EBI University of Minnesota
9804688 51 Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.EBI University of Minnesota
9719602 24 3-Alkyl ethers of clocinnamox: delayed long-term mu-antagonists with variable mu efficacy.EBI University of Bristol
9667975 86 Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.EBI Southern Research Institute
9651168 12 Synthesis and biological activity of a novel methylamine-bridged enkephalin analogue (MABE): a new route to cyclic peptides and peptidomimetics.EBI University of California at San Diego
9057861 33 (E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.EBI University of Washington
9379438 31 Discovery of a novel class of substituted pyrrolooctahydroisoquinolines as potent and selective delta opioid agonists, based on an extension of the message-address concept.EBI SmithKline Beecham S.p.A.
9288176 95 Probes for narcotic receptor-mediated phenomena. 25. Synthesis and evaluation of N-alkyl-substituted (alpha-piperazinylbenzyl)benzamides as novel, highly selective delta opioid receptor agonists.EBI National Institute of Diabetes and Digestive and Kidney Diseases
9207938 15 Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.EBI University of Minnesota
9171881 17 7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.EBI University of Minnesota
8627605 10 Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide"address" recognition at kappa opioid receptors.EBI University of Minnesota
8648612 30 Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.EBI University of Minnesota
8642567 64 Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.EBI National Institute of Diabetes and Digestive and Kidney Diseases
7739013 26 Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.EBI Research Triangle Institute
7739011 90 Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.EBI National Institute of Diabetes and Digestive and Kidney Diseases
7853350 33 Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.EBI University of Washington
7853332 27 7'-Substituted amino acid conjugates of naltrindole. Hydrophilic groups as determinants of selective antagonism of delta 1 opioid receptor-mediated antinociception in mice.EBI University of Minnesota
7636870 18 Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.EBI University of Innsbruck
8126697 30 Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.EBI University of Minnesota
7996538 42 Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.EBI University of Washington
7932569 116 Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.EBI Virginia Commonwealth University
8071934 30 Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.EBI University of Washington
8021929 13 Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.EBI University of Minnesota
7515442 9 14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.EBI Institute
8182708 18 Structure-activity relationship of N17'-substituted norbinaltorphimine congeners. Role of the N17' basic group in the interaction with a putative address subsite on the kappa opioid receptor.EBI University of Minnesota
8394935 4 A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.EBI University of Minnesota
8360887 9 Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.EBI University of Minnesota
8393489 25 A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.EBI Glaxo Group Research Ltd.
8390575 28 Non-peptide ligands for opioid receptors. Design of kappa-specific agonists.EBI Universit£ di Catania
8380614 6 A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.EBI University of Minnesota
1315870 39 Substitution on the Phe3 aromatic ring in cyclic delta opioid receptor-selective dermorphin/deltorphin tetrapeptide analogues: electronic and lipophilic requirements for receptor affinity.EBI University of Michigan
1361580 19 N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.EBI Oregon State University
1335078 57 O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.EBI University of Washington
1333014 12 Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.EBI University of Michigan
1333013 24 Opioid agonist and antagonist activities of morphindoles related to naltrindole.EBI University of Minnesota
1323679 21 Substituted 1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for kappa and mu opioid receptors.EBI Zambeletti Research Laboratories
1322988 60 Probes for narcotic receptor mediated phenomena. 18. Epimeric 6 alpha- and 6 beta-iodo-3,14-dihydroxy-17-(cyclopropylmethyl)-4,5 alpha-epoxymorphinans as potential ligands for opioid receptor single photon emission computed tomography: synthesis, evaluation, and radiochemistry of [125I]-6 beta-iodoEBI National Institute of Diabetes and Digestive and Kidney Diseases
1320121 36 Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.EBI University of Washington
1319495 21 Selective reversible and irreversible ligands for the kappa opioid receptor.EBI National Taiwan University
1319493 27 Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.EBI National Institute of Diabetes and Digestive and Kidney Diseases
1648136 12 An approach to the design of receptor-type-selective non-peptide antagonists of peptidergic receptors: delta opioid antagonists.EBI University of Minnesota
1851846 3 Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.EBI University of Minnesota
1849995 12 Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.EBI University of Minnesota
1659636 51 Structure/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists.EBI ICI Pharmaceuticals
1846919 20 Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.EBI Parke-Davis Research Unit
2167979 31 Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.EBI Universit£ Louis Pasteur
2160538 81 Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.EBI University of Minnesota
2172538 58 Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.EBI National Institute of Diabetes and Digestive and Kidney Diseases
2153208 3 Highly selective kappa-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives.EBI Parke-Davis Research Unit
2549247 39 Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.EBI CIBA-GEIGY Corporation
2547074 16 Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.EBI National Institute of Digestive
2567782 50 Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.EBI Parke-Davis Research Unit
2542556 65 Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.EBI Ciba-Geigy Corporation
2536436 23 Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.EBI Smith Kline and French Laboratories
2832603 63 Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.EBI Parke-Davis Research Unit
2831363 18 Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.EBI Eli Lilly and Company
2845084 22 Effects of addition of a 2-methyl group to ethyl nipecotates (beta-meperidines) on receptor affinities and opiate agonist/antagonist activities.EBI SRI International
2887656 48 Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.EBI TBA
2879914 30 Peptides as receptor selectivity modulators of opiate pharmacophores.EBI TBA
3007760 44 N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.EBI TBA
2409281 9 10-Ketonaltrexone and 10-ketooxymorphone.EBI TBA
14980696 47 Design and synthesis of novel small molecule N/OFQ receptor antagonists.EBI Purdue Pharma L.P.
15203136 37 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
14684324 27 The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.EBI SRI International
12565965 45 Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.EBI Southern Research Institute
14643346 65 trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.EBI Adolor Corporation
12372523 133 Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.EBI Schering Plough Research Institute
11294396 57 Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.EBI University of Bristol
11597422 39 Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.EBI NIDDK
11591513 87 Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.EBI Harvard Medical School
11425545 22 3-Carboxamido analogues of morphine and naltrexone. synthesis and opioid receptor binding properties.EBI Pharmacia
10782696 64 ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.EBI F. Hoffmann-La Roche Ltd.
10743951 5 Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.EBI Albany Molecular Research
11078198 12 N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.EBI University of Maryland
11055333 21 Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.EBI University of Bristol
10673107 48 8-Aminocyclazocine analogues: synthesis and structure-activity relationships.EBI Institute
10340622 47 Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.EBI Organon Laboratories Ltd.
10206545 40 Ring constrained analogues of the orvinols: the furanomorphides.EBI University of Bristol
10617086 21 Delta opioid binding selectivity of 3-ether analogs of naltrindole.EBI National Institute of Diabetes
10612597 31 Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.EBI Research Triangle Institute
10571174 25 (+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.EBI Research Triangle Institute
9871544 24 Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.EBI National Institute of Diabetes
9873603 23 Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.EBI University of Michigan
9873480 35 Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.EBI Institute for Bioorganic Research
 33 Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studiesEBI TBA
 17 Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivityEBI TBA
 9 Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodimeEBI TBA
 49 EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonistsEBI TBA
 21 Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogsEBI TBA
 16 DuP 747: a new, potent, kappa opioid analgesic. Synthesis and pharmacology1.EBI TBA
22341895 26 Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selectiveµ-antagonist activity.EBI National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism
22284817 82 ¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.EBI AstraZeneca R&D Montreal
22204910 17 Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.EBI Harvard Medical School
22136765 31 Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.EBI Institute of Radiopharmacy
22197670 51 Synthesis of quinolinomorphinan-4-ol derivatives asd opioid receptor agonists.EBI Kitasato University
21958337 54 Discovery of aminobenzyloxyarylamides as¿ opioid receptor selective antagonists: application to preclinical development of a¿ opioid receptor antagonist receptor occupancy tracer.EBI Lilly Research Laboratories
21967807 36 Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.EBI University of Pavia
21905669 9 Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.EBI University of Illinois at Chicago
21889335 27 Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).EBI Kitasato University
21866885 71 Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.EBI University of Bath
21788137 33 N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI The University of Sydney
21788135 40 Structure selectivity relationship studies of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6ß-[(4'-pyridyl)carboxamido]morphinan derivatives toward the development of the mu opioid receptor antagonists.EBI Virginia Commonwealth University
21744827 76 Design and discovery of a selective small molecule¿ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).EBI Pfizer Inc.
21667972 5 Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.EBI The University of Mississippi
21570305 13 Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.EBI National Institute on Drug Abuse and The National Institute on Alcohol Abuse and Alcoholism
21684752 25 Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.EBI National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism
21641219 12 Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.EBI Kitasato University
21481987 27 Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.EBI Institut f£r Pharmazeutische und Medizinische Chemie der Universit£t M£nster
21413804 21 Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.EBI Vrije Universiteit Brussel
21482470 71 Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.EBI Harvard Medical School
21338114 27 Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.EBI University of Iowa
21392859 1 Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor.EBI Indian Institute of Chemical Biology
21330016 96 Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.EBI Istituto Superiore di Sanit£
21256034 58 Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.EBI Kitasato University
21247164 37 Probes for narcotic receptor mediated phenomena. 41. Unusual inverseµ-agonists and potentµ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.EBI National Institute on Drug Abuse
21235243 35 Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.EBI University of Innsbruck
21126878 21 Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.EBI Institut f£r Pharmazeutische und Medizinische Chemie der Universit£t M£nster
21115248 11 Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.EBI University of Mississippi
20850307 27 Design and synthesis of KNT-127, ad-opioid receptor agonist effective by systemic administration.EBI Kitasato University
20812727 157 Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI National Institute of Mental Health
20801035 22 Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.EBI Harvard Medical School
20727752 141 Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.EBI AstraZeneca Pharmaceuticals
20692738 34 Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.EBI "Sapienza" Università di Roma
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20681583 7 Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.EBI Hokkaido University
20719509 93 SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.EBI AstraZeneca Pharmaceuticals
20709559 16 Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.EBI Purdue University
20685120 20 Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.EBI Kitasato University
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
20483601 22 Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.EBI Kitasato University
20426456 12 Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.EBI Griffith University
20144870 51 Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.EBI Harvard Medical School
20144865 18 Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.EBI Kyorin Pharmaceutical Co., Ltd
20137933 218 Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.EBI Amgen Inc.
19818611 100 Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.EBI Schering-Plough Research Institute
19767206 9 Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.EBI National Institute of Mental Health
19647430 104 N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.EBI Pfizer Global Research and Development
20056539 14 Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.EBI Kitasato University
20045339 16 Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).EBI University of Pavia
20005115 26 Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols.EBI NIDA
20015649 53 Biaryl piperidines as potent and selective delta opioid receptor ligands.EBI Pfizer Global Research and Development
19963374 68 Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.EBI Pfizer Global Research and Development
19932964 26 Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.EBI Fudan University
19646882 72 Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and the Informatics Institute of UMDNJ
19640720 4 Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.EBI Institute of Chemical Biology
20055417 62 Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.EBI National Taiwan University
19928862 120 Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.EBI Harvard Medical School
19800791 98 N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: the development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models.EBI AstraZeneca R&D Montr£al
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19694469 3 Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.EBI Biomedizinische Forschungsreagenzien GmbH
19634902 55 Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.EBI Harvard Medical School
19627147 27 Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans.EBI National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholi
19842669 34 14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.EBI University of Bristol
19827750 39 Agonist vs antagonist behavior of delta opioid peptides containing novel phenylalanine analogues in place of Tyr(1).EBI Clinical Research Institute of Montreal
19807094 45 The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.EBI University of Kansas
19800790 62 Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability.EBI AstraZeneca R&D Montr£al
19791807 18 Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.EBI Institut f£r Pharmazeutische und Medizinische Chemie der Westf£lischen Wilhelms-Universit£t M£nster
19788201 32 Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.EBI University of Michigan
19576786 129 Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands.EBI Institute for Molecular Studies
19364645 15 Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.EBI University of New England
19715279 20 Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.EBI The University of Kansas
19694468 136 Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).EBI Adolor Corporation
19620007 4 Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.EBI Kitasato University
19564110 31 Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.EBI Tsukuba Research Institute
19537798 22 Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.EBI Tsukuba Research Institute
 17 trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonistsEBI TBA
 21 Arylacetamide kappa-selective opioid ligandsEBI TBA
 26 6N-Cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actionsEBI TBA
 12 Synthesis and opioid binding properties of 2-chloroacrylamido derivatives of 7,8-dihydromorphinansEBI TBA
 5 Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)EBI TBA
 35 Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective μ-opioid analgesicEBI TBA
 24 Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonistsEBI TBA
 13 N-Methyl and N-cyclopropylmethyl-14α,14′β-[dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydro-5β-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: Synthesis and opioid binding propertiesEBI TBA
 9 Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogsEBI TBA
 22 Palladium-catalyzed synthesis of C3-substituted 3-deoxymorphines.EBI TBA
 8 The design and synthesis of kappa opioid ligands based on a binding model for kappa agonistsEBI TBA
 6 New potent enkephalin analogs containing trifluoromethylamino acid residuesEBI TBA
 13 Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective κ-opioid receptor agonistsEBI TBA
19339177 127 The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.EBI Schering-Plough Research Institute
19332374 84 Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.EBI Schering-Plough Research Institute
19253970 39 Mixed kappa/mu opioid receptor agonists: the 6 beta-naltrexamines.EBI University of Bath
19168350 58 Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.EBI University of Toronto
19147366 60 Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.EBI McLean Hospital
19091564 41 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.EBI Rensselaer Polytechnic Institute
19053757 25 Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of the ortho- and para-d-isomers.EBI National Institute on Drug Abuse
18800771 26 Novel opioid peptide derived antagonists containing (2S)-2-methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid [(2S)-Mdcp].EBI National University of Singapore
18701276 97 Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI Merck Research Laboratories
18674902 48 Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.EBI Harvard Medical School
18674898 35 Aminomethylpiperazines as selective urotensin antagonists.EBI GlaxoSmithKline Pharmaceuticals
18537234 55 A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.EBI Tsukuba Research Institute
18524591 62 Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.EBI GlaxoSmithKline Pharmaceuticals
18515099 12 Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.EBI Tsukuba Research Institute
18499305 11 1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.EBI Institut für Pharmazeutische und Medizinische Chemie
18448337 31 Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.EBI Banyu Tsukuba Research Institute
17988766 26 Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.EBI University of Maryland
16792410 48 Synthesis of salvinorin A analogues as opioid receptor probes.EBI The University of Iowa
16441078 4 Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A.EBI The University of Iowa
18067245 11 Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.EBI National Institute of Mental Health
17904842 4 Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.EBI Holden Laboratories
17826993 17 5'-halogenated analogs of oxymorphindole.EBI University of Maryland
17720493 93 Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.EBI Lilly Research Laboratories
17625813 33 Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.EBI National Institute on Drug Abuse
17601735 24 Functionalization of the 6,14-bridge of the orvinols. Part 3: preparation and pharmacological evaluation of 18- and 19-hydroxyl substituted orvinols.EBI University of Maryland
17583504 51 Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17571866 49 Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI National Institute of Mental Health
17548197 3 4-Amino-5-vinyl-3(2H)-pyridazinones and analogues as potent antinociceptive agents: Synthesis, SARs, and preliminary studies on the mechanism of action.EBI Dipartimento di Scienze Farmaceutiche
17512730 95 4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.EBI Johnson & Johnson Pharmaceutical Research & Development
17497839 72 Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.EBI Kobe Gakuin University
17488103 56 Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.EBI Chinese Academy of Sciences
17433695 54 In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.EBI Harvard Medical School
17420123 219 Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.EBI Schering-Plough Research Institute
17350835 88 Further studies of tyrosine surrogates in opioid receptor peptide ligands.EBI Adolor Corporation
17315860 40 Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.EBI Clinical Research Institute of Montreal
17307360 20 Novel malonamide derivatives as potent kappa opioid receptor agonists.EBI Adolor Corporation
17303418 8 Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.EBI University of Mississippi
17289383 157 Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.EBI Schering Plough Research Institute
17166723 141 Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.EBI Organon Laboratories Ltd.
16945525 32 Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.EBI Harvard Medical School
16942040 12 New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.EBI Harvard Medical School
16913729 9 Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.EBI National University of Singapore
16777411 80 Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).EBI McLean Hospital
16750366 104 Identification of potent and highly selective chiral tri-amine and tetra-amine mu opioid receptors ligands: an example of lead optimization using mixture-based libraries.EBI Institute for Molecular Studies
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Global Research & Development
16632355 116 3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.EBI Johnson & Johnson Pharmaceutical Research and Development
16621556 12 Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.EBI The University of Iowa
16458504 37 Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI Columbia University College of Physicians and Surgeons
16451050 111 Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.EBI Banyu Tsukuba Research Institute
16392798 46 Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI Columbia University College of Physicians and Surgeons
16298525 96 Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.EBI Adolor Corporation
16263278 46 Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.EBI Adolor Corporation
16236510 85 4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.EBI Johnson and Johnson Pharmaceutical Research and Development
16203140 74 Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.EBI Adolor Corporation
16153834 102 Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.EBI Johnson & Johnson Pharmaceutical Research and Development
16143528 213 Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI Columbia University College of Physicians and Surgeons
16051487 42 Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.EBI Harvard Medical School
16033256 57 Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.EBI The University of Iowa
15863335 111 Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.EBI Adolor Corporation
15713370 22 Amino acid conjugates as kappa opioid receptor agonists.EBI Adolor Corporation
15686919 12 Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.EBI Adolor Corporation
15658846 13 Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.EBI The University of Melbourne
15482950 17 Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.EBI Adolor Corporation
15456245 44 Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.EBI Johnson & Johnson Pharmaceutical Research & Development
15324897 3 A novel cyclic enkephalin analogue with potent opioid antagonist activity.EBI Clinical Research Institute of Montreal
15163203 45 Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.EBI University of Innsbruck
15163178 70 A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.EBI SRI International
15027881 32 Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.EBI Vrije Universiteit Brussel
14736254 70 Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.EBI Biological Research Center of the Hungarian Academy of Sciences
14711314 63 Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.EBI University of Maryland
14695830 111 10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.EBI Harvard Medical School
12954053 39 Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.EBI University of Maryland
12951102 46 Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.EBI Purdue Pharma L.P.
12749896 47 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.EBI Rensselaer Polytechnic Institute
12699761 84 New scaffolds in the development of mu opioid-receptor ligands.EBI AstraZeneca R&D Montreal
12672238 3 Mechanism of action of the diazabicyclononanone-type kappa-agonists.EBI Universität Würzburg
12672226 9 A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.EBI University of Maryland
12643930 93 Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.EBI AstraZeneca R&D
12593663 146 Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.EBI Rensselaer Polytechnic Institute
12477343 8 Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.EBI University of Maryland
12408719 21 Synthesis and structure-activity relationships of an orally available and long-acting analgesic peptide, N(alpha)-amidino-Tyr-D-Arg-Phe-MebetaAla-OH (ADAMB).EBI Daiichi Fine Chemical Co. Ltd.
12383009 2 Kappa-opioid receptor model in a phospholipid bilayer: molecular dynamics simulation.EBI University of Catania
12372527 27 Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.EBI Institute for Molecular Studies
12372519 22 Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.EBI Shire Biochem
12190304 10 Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.EBI University of Maryland
12166947 30 Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.EBI University of California
12161117 2 3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.EBI Chinese Academy of Sciences
11755353 61 3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.EBI AstraZeneca R&D Mölndal
11755345 18 Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.EBI NIDDK
11448220 93 Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.EBI AstraZeneca R&D Montreal
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
11266156 42 8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.EBI Rensselaer Polytechnic Institute
11212101 8 Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.EBI Clinical Research Institute of Montreal
11150174 84 Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.EBI Virginia Commonwealth University
11101358 24 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.EBI Central Pharmaceutical Research Institute
11086731 16 Arylacetamides as peripherally restricted kappa opioid receptor agonists.EBI Adolor Corporation
11052794 103 N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.EBI AstraZeneca R&D Montreal
11052793 115 New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.EBI AstraZeneca R&D Montreal
11020289 9 Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones.EBI University of Würzburg
10893314 24 Potent and selective indolomorphinan antagonists of the kappa-opioid receptor.EBI University of Minnesota
10866400 18 4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.EBI Research Triangle Institute
10841790 24 Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.EBI Istituto di Chimica Farmaceutica e Tossicologica
10741545 36 Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.EBI Pfizer Inc
10673103 55 Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.EBI AstraZeneca R&D Montréal
10612602 29 Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.EBI University of Illinois at Chicago
10602690 36 Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
10479285 17 The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.EBI Clinical Research Institute of Montreal
10447942 9 A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.EBI TBA
10340623 29 Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.EBI Organon Laboratories Ltd.
9873693 24 N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.EBI Research Triangle Institute
9873439 16 C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.EBI National Taiwan University
9767649 24 N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.EBI Research Triangle Institute
9599247 57 Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.EBI Research Triangle Institute
9301669 24 7-spirobenzocyclohexyl derivatives of naltrexone, oxymorphone, and hydromorphone as selective opioid receptor ligands.EBI University of Minnesota
9276018 47 Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.EBI Oregon State University
9111295 48 Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.EBI Oregon State University
9083489 30 Conformationally constrained deltorphin analogs with 2-aminotetralin-2-carboxylic acid in position 3.EBI Hungarian Academy of Sciences
8893842 6 Aspartic acid conjugates of 2-(3,4-dichlorophenyl)-N-methyl-N-[(1S)-1(3-aminophenyl)-2-(1-pyrrolidi nyl) ethyl]acetamide: kappa opioid receptor agonists with limited access to the central nervous system.EBI University of Minnesota
8691442 52 Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.EBI University of Arizona
8676350 39 Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.EBI University of Arizona
8642554 42 Asymmetric syntheses, opioid receptor affinities, and antinociceptive effects of 8-amino-5,9-methanobenzocyclooctenes, a new class of structural analogues of the morphine alkaloids.EBI Institute
8632410 33 Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.EBI Universitá di Siena
8558529 195 Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.EBI Hoechst-Roussel Pharmaceuticals Inc.
8410999 73 3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI Lilly Research Laboratories
8410998 127 Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.EBI Lilly Research Laboratories
8246239 71 Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI Solvay Duphar B.V.
8201586 3 2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice.EBI University of Minnesota
8097539 10 Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.EBI Oregon State University
8096246 70 Design and synthesis of highly potent and selective cyclic dynorphin A analogs. 2. New analogs.EBI University of Arizona
8057274 18 Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.EBI Lilly Research Laboratories
8035420 13 4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists.EBI Glaxo Group Research Ltd.
7966152 57 Design, synthesis, and biological properties of highly potent cyclic dynorphin A analogues. Analogues cyclized between positions 5 and 11.EBI University of Arizona
7932577 24 Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.EBI SmithKline Beecham Farmaceutici S.p.A.
7932540 38 A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.EBI National Institute of Diabetes and Digestive and Kidney Diseases
7932535 40 Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.EBI National Taiwan University
7908696 45 Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide.EBI Searle
7861405 9 Highly kappa receptor-selective dynorphin A analogues with modifications in position 3 of dynorphin A(1-11)-NH2.EBI University of Arizona
7799399 8 kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists.EBI University of Minnesota
7731019 16 Electrophilic N-benzylnaltrindoles as delta opioid receptor-selective antagonists.EBI University of Minnesota
7707326 39 Opioid receptor binding requirements for the delta-selective peptide deltorphin. I: Phe3 replacement with ring-substituted and heterocyclic amino acids.EBI Eastern Michigan University
7693944 51 14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity.EBI Institute
7658433 27 Synthesis using a Fmoc-based strategy and biological activities of some reduced peptide bond pseudopeptide analogues of dynorphin A1.EBI University of Arizona
7608905 24 Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the"message" sequence.EBI Oregon State University
7490727 72 (E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.EBI National Institute of Diabetes and Digestive and Kidney Diseases
6313921 9 Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.EBI TBA
3020244 45 Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.EBI TBA
2876099 51 Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.EBI TBA
1972964 24 Design and synthesis of highly potent and selective cyclic dynorphin A analogues.EBI University of Arizona
1967312 91 Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.EBI Eisai Co., Ltd.
1895300 15 Modification of the enkephalin"message" with an artificial polycationic C-terminus.EBI Case Western Reserve University
1847432 13 New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.EBI Anaquest, Inc.
1846921 49 (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.EBI Zambeletti Research Laboratories
1846918 12 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists.EBI ICI Pharmaceuticals
1652025 42 (1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.EBI Zambeletti Research Laboratories
1652019 10 Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.EBI University of Washington
1648141 21 Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.EBI University of Notre Dame
1360025 27 Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.EBI Oregon State University
1346276 25 Preparation and opioid activity of analogues of the analgesic dipeptide 2,6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide.EBI G. D. Searle and Company
1315868 34 Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.EBI Harvard Medical School
1310743 38 New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus.EBI Glaxo Group Research Ltd.
24121503 231 Chemotype-selective modes of action of ┐-opioid receptor agonists.BDB University of North Carolina School of Medicine
23775075 6 Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at kappa-opioid receptors in striatal neurons.BDB The Scripps Research Institute
19337725 43 Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.BDB Case Western Reserve University
18313920 74 Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.BDB Adolor Corporation
18311899 26 Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.BDB University of Maryland
18298057 83 Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.BDB Human BioMolecular Research Institute
17221184 55 Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.BDB Columbia University
16915381 31 WAY-100635 is a potent dopamine D4 receptor agonist.BDB Purdue University
16352709 44 Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.BDB McGill University
16076937 5 Characterization of a novel bivalent morphinan possessing kappa agonist and micro agonist/antagonist properties.BDB University of Rochester
15952771 5 Identification of the molecular mechanisms by which the diterpenoid salvinorin A binds to kappa-opioid receptors.BDB Case Western Reserve University
15509719 17 [(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a highly potent and selective agonist of the nociceptin/orphanin FQ receptor.BDB Section of Pharmacology
15383632 15 Comparison of pharmacological activities of three distinct kappa ligands (Salvinorin A, TRK-820 and 3FLB) on kappa opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo.BDB Temple University
15178355 19 Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine.BDB Memorial Sloan-Kettering Cancer Center
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
15054115 11 DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.BDB Purdue Pharma Discovery Research
14993260 2 FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity.BDB University of Arizona
14729121 29 In vitro opioid activity profiles of 6-amino acid substituted derivatives of 14-O-methyloxymorphone.BDB University of Innsbruck
14534366 25 Comparison of [Dmt1]DALDA and DAMGO in binding and G protein activation at mu, delta, and kappa opioid receptors.BDB Cornell University
12887410 15 Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist.BDB University of Innsbruck
12842269 16 Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.BDB University of Michigan
12784105 53 Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.BDB Case Western Reserve University
12649361 779 L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.BDB Case Western Reserve University
12431845 84 Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.BDB Lilly Research Laboratories
12192085 52 Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.BDB Case Western Reserve University
12110997 380 In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.BDB Westfälische Wilhelms-Universitä Muenster,
12065740 8 8-Carboxamidocyclazocine: a long-acting, novel benzomorphan.BDB University of Rochester
11750183 29 Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.BDB Novartis Pharma
11750180 139 Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.BDB Lilly Research Laboratories
11512051 80 The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.BDB Case Western Reserve University
11438309 51 The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.BDB Janssen Research Foundation
11270320 11 Dynorphin A analogs containing a conformationally constrained phenylalanine derivative in position 4: reversal of preferred stereochemistry for opioid receptor affinity and discrimination of kappa vs. delta receptors.BDB University of Maryland
11191833 15 Characterisation and comparison of novel ligands for the nociceptin/orphanin FQ receptor.BDB Leicester Royal Infirmary
11121615 32 Synthesis and in vitro opioid activity profiles of DALDA analogues.BDB Clinical Research Institute of Montreal
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
10585536 23 Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.BDB Hungarian Academy of Sciences
10565829 17 Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.BDB Loughborough University
10374926 2 Opioid binding profiles of new hydrazone, oxime, carbazone and semicarbazone derivatives of 14-alkoxymorphinans.BDB Hungarian Academy of Sciences
10087018 11 Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.BDB University of Rochester
9700760 21 Interaction of agonist peptide [3H]Tyr-D-Ala-Phe-Phe-NH2 with mu-opioid receptor in rat brain and CHO-mu/1 cell line.BDB Hungarian Academy of Sciences
9694962 65 Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain.BDB Memorial Sloan-Kettering Cancer Center
9686407 633 Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.BDB SRI International
9225287 174 RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.BDB Roche Bioscience
8935801 586 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.BDB Janssen Research Foundation
8887981 72 A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.BDB Abbott Laboratories
8564266 77 Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.BDB Vrije Universiteit
8114680 110 Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.BDB University of Pennsylvania
8012715 38 GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.BDB Glaxo Group Research Ltd.
7932177 53 Biochemical and pharmacological characterization of mu, delta and kappa 3 opioid receptors expressed in BE(2)-C neuroblastoma cells.BDB Memorial Sloan-Kettering Cancer Center
7910212 34 Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.BDB Yamanouchi Pharmaceutical Co. Ltd.
7562497 127 Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.BDB R.W. Johnson Pharmaceutical Research Institute
2531826 24 [125]I-spectramide: a novel benzamide displaying potent and selective effects at the D2 dopamine receptor.BDB NIDA Addiction Research Center
2177154 43 Characterization of kappa 1 and kappa 2 opioid binding sites in frog (Rana esculenta) brain membrane preparation.BDB Biological Research Center of Hungarian Academy of Sciences
1982626 30 Neurochemical profile of eltoprazine.BDB Duphar B.V.
1661335 95 Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.BDB Center for Bio-Pharmaceutical Sciences
19041249 48 Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists.BDB Nippon Shinyaku Co.
19147350 264 Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: part 2.BDB Schering-Plough Research Institute
18232652 84 Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.BDB Istituto Superiore di Sanita
17539621 17 Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.BDB Universita degli Studi