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438 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28318942 10 Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.EBI Medical University of Lodz
28011222 16 Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.EBI West Virginia University School of Pharmacy
28051300 74 Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.EBI University of Tsukuba
27776274 81 Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists.EBI National Health Research Institutes
1310115 11 Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols.EBI Glaxo Group Research Ltd.
2475628 5 Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.EBI University of Minnesota
2872334 16 Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.EBI TBA
3020245 4 Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.EBI TBA
6312042 7 Different receptor sites mediate opioid agonism and antagonism.EBI TBA
6283082 3 Stereochemical studies on medicinal agents. 25. Absolute configuration and analgetic potency of beta-1,2-dimethyl-2-phenyl-4-(propionyloxy)piperidine enantiomers.EBI TBA
6106064 20 Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.EBI TBA
10476866 3 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.EBI F. Hoffmann-La Roche Ltd
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
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
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
27079125 56 Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.EBI Kitasato University
27043173 47 Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure-activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives.EBI Pfizer Inc.
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
26819673 55 Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.EBI AstraZeneca
26390077 42 Tactical Approaches to Interconverting GPCR Agonists and Antagonists.EBI University of Minnesota
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
26632862 20 Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting theÁ-Opioid Receptor.EBI University of Nottingham
26403932 9 Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.EBI Lanzhou University
26348881 54 Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.EBI National Health Research Institutes
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
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
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
26005537 72 Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.EBI Medical University of Lodz
25901762 33 Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of thed-opioid receptor.EBI Bristol-Myers Squibb Company
25494650 8 CNS drug design: balancing physicochemical properties for optimal brain exposure.EBI Eli Lilly and Company
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
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
25782742 76 trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.EBI Novartis Pharma AG
25754490 44 trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.EBI Novartis Pharma AG
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
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
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
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
24871036 13 4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.EBI AstraZeneca
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
24697290 6 Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.EBI University of Texas Southwestern Medical Center
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.
24900842 71 Novel delta opioid receptor agonists with oxazatricyclodecane structure.EBI Kitasato University
24613457 64 Endomorphin analogues with mixedÁ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lacking▀-arrestin2 recruitment activity.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
24332089 35 Imidazole-derived agonists for the neurotensin 1 receptor.EBI Conrad Prebys Center for Chemical Genomics at Sanford-Burnham Medical Research Institute
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
23548164 1 Neoclerodanes as atypical opioid receptor ligands.EBI University of Kansas
23477419 64 Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.EBI Lanzhou University
23360448 18 Development of¿ opioid receptor antagonists.EBI Research Triangle Institute
23281966 8 Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.EBI AstraZeneca
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
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
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
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
21354674 14 The many faces of the adamantyl group in drug design.EBI University of Sydney
22724433 76 A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).EBI Lanzhou University
23022277 13 Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.EBI The University of Queensland
23017884 4 Formylated polyamines as peptidomimetics.EBI The Scripps Research Institute
22771010 3 An efficient synthesis of 3-OBn-6ß,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.EBI University of New England
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
22898529 58 Discovery of 1-(ß-amino substituted-ß-alanyl)-N,N-dimethylindoline-2-carboxamides as novel nonpeptide antagonists of nociceptin/orphanin FQ receptor: efficient design, synthesis, and structure-activity relationship studies.EBI Pfizer Inc.
22439881 157 Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.EBI Harvard Medical School
24900459 53 NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with Á-Opioid Agonist Activity.EBI TBA
22542010 31 Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI Amgen San Francisco
22464684 85 Semisynthetic neoclerodanes as kappa opioid receptor probes.EBI The University of Kansas
21621410 44 Generation of novel radiolabeled opiates through site-selective iodination.EBI Memorial Sloan-Kettering Cancer Center
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
20599386 46 Evaluation of N-substitution in 6,7-benzomorphan compounds.EBI University of Catania
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
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
19683449 116 Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.EBI Human BioMolecular Research Institute
19700325 46 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).EBI Sepracor Inc.
19595591 37 Synthesis and opioid receptor activity of indolopropellanes.EBI Chinese Academy of Sciences
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
19253983 37 14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.EBI University of Bath
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
18637671 21 Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.EBI Toray Industries, Inc
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
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
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
18243691 18 Potent, selective MCH-1 receptor antagonists.EBI Hoffmann-La Roche, Inc.
18242987 75 In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.EBI Sepracor Inc.
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
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
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
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
16762550 101 4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.EBI F. Hoffmann-La Roche Ltd
16821764 54 Discovery of novel triazole-based opioid receptor antagonists.EBI University of Medicine and Dentistry of New Jersey and UMDNJ Informatics Institute
16789756 25 New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.EBI Vrije Universiteit Brussels
16257206 18 Derivatives of tramadol for increased duration of effect.EBI Sepracor Inc.
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
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15743177 43 Synthesis and biological evaluation of meperidine analogues at monoamine transporters.EBI University of New Orleans
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
15745801 5 Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.EBI Human BioMolecular Research Institute
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
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
13678399 54 Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.EBI University of Arizona
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
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
12747782 79 Structure-activity relationships of dynorphin a analogues modified in the address sequence.EBI University of California
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
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
12086475 1 Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties.EBI University of Minnesota
11297446 3 Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).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
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.
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
10966754 9 3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.EBI University of Bristol
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
10891118 6 Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.EBI University of Northern Colorado
10891107 3 Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.EBI University of Minnesota
10229619 4 Emerging molecular approaches to pain therapy.EBI Abbott Laboratories
10508425 68 Mixture-based synthetic combinatorial libraries.EBI Torrey Pines Institute for Molecular Studies
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
9301674 60 Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.EBI University of Ferrara
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
9171881 17 7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.EBI University of Minnesota
8126697 30 Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.EBI University of Minnesota
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
1361580 25 N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.EBI Oregon State University
1335078 76 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
1320121 48 Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.EBI University of Washington
2153826 11 Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.EBI University of Washington
2213824 20 Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.EBI Pfizer central Research
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
14980696 47 Design and synthesis of novel small molecule N/OFQ receptor antagonists.EBI Purdue Pharma L.P.
15203136 39 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
14684324 46 The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.EBI SRI International
12643904 12 Synthesis and binding affinity of neuropeptide Y at opiate receptors.EBI University of North Carolina at Wilmington
14643346 65 trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.EBI Adolor Corporation
12372523 134 Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.EBI Schering Plough Research Institute
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
11055333 21 Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.EBI University of Bristol
10206545 40 Ring constrained analogues of the orvinols: the furanomorphides.EBI University of Bristol
9873602 11 A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.EBI University of Michigan
 16 DuP 747: a new, potent, kappa opioid analgesic. Synthesis and pharmacology1.EBI TBA
22357342 8 SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives asµ opioid ligands.EBI Pfizer Inc.
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
22197137 61 4-Piperidin-4-ylidenemethyl-benzamides asd-opioid receptor agonists for CNS indications: identifying clinical candidates.EBI AstraZeneca Pharmaceuticals
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
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
21870874 30 Synthesis, biological evaluation, and automated docking of constrained analogues of the opioid peptide H-Dmt-D-Ala-Phe-Gly-NH2 using the 4- or 5-methyl substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one scaffold.EBI Vrije Universiteit Brussel
21866885 71 Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.EBI University of Bath
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
21737265 2 Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a 'magic methyl' giving a 35-fold improvement in binding.EBI Pfizer Inc.
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
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
21330016 96 Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.EBI Istituto Superiore di Sanit£
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
20980153 83 Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.EBI University of New Orleans
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
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
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
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
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
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
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
20047331 30 Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.EBI Solvay Pharma
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
19679474 8 Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.EBI Lanzhou University
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
19621878 19 Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.EBI The University of Kansas
19842669 34 14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.EBI University of Bristol
19836950 9 Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.EBI Aix-Marseille Universit£
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
19364645 15 Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.EBI University of New England
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
19564110 31 Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.EBI Tsukuba Research Institute
19678644 52 Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.EBI Schering-Plough 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
8496700 16 The Role of Receptor Binding in Drug DiscoveryEBI TBA
 37 The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.EBI TBA
 8 The design and synthesis of kappa opioid ligands based on a binding model for kappa 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
19329329 183 Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
19231185 44 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.EBI Pfizer Global Research and Development
19168350 58 Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.EBI University of Toronto
19113864 27 Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.EBI University of Minnesota
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
18990569 76 Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.EBI Schering-Plough Research Institute
18783208 11 Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI National Institute of Mental Health
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
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc.
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
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
18468445 26 Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.EBI University of Queensland
18448337 31 Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.EBI Banyu Tsukuba Research Institute
18329886 15 Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues.EBI University of Queensland
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
18207400 17 Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.EBI Medical University of Lodz
17826995 48 Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.EBI Kobe Gakuin University
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
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
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
17289383 157 Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.EBI Schering Plough Research Institute
17266203 29 Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).EBI Medical University
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.
16942040 12 New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.EBI Harvard Medical School
16762548 37 Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.EBI F. Hoffmann-La Roche Ltd
16757170 40 Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.EBI F. Hoffmann-La Roche Ltd
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Global Research & Development
16722631 87 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.EBI Predix Pharmaceuticals Ltd.
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
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
16361098 70 Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.EBI F. Hoffmann-La Roche Ltd
16302812 6 Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents.EBI Technische Universität München
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
16275086 18 Synthesis and biological activity of the first cyclic biphalin analogues.EBI University of Arizona
16263278 46 Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.EBI Adolor Corporation
16246561 90 Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.EBI F. Hoffmann-La Roche Ltd
16246557 75 Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.EBI F. Hoffmann-La Roche Ltd
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
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
15664818 81 Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.EBI Organon Laboratories Ltd
15482950 17 Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.EBI Adolor Corporation
15454210 36 Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.EBI Purdue Pharma L.P.
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
15080990 92 N-alkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, micro and delta opioid agonists: a micro address.EBI Johnson and Johnson Pharmaceutical Research and Development
15080989 107 N,N-dialkyl-4-[(8-azabicyclo[3.2.1]-oct-3-ylidene)phenylmethyl]benzamides, potent, selective delta opioid agonists.EBI Johnson and Johnson Pharmaceutical Research and Development
14698188 13 Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: a new series of hybrid molecules with significant binding affinity for mu-opioid receptors and I2-imidazoline binding sites.EBI Instituto de Química Médica
12951102 46 Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.EBI Purdue Pharma L.P.
12699761 85 New scaffolds in the development of mu opioid-receptor ligands.EBI AstraZeneca R&D Montreal
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 95 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
12372519 22 Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.EBI Shire Biochem
12166947 30 Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.EBI University of California
11755353 61 3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.EBI AstraZeneca R&D Mölndal
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
11356103 61 Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.EBI SmithKline Beecham Pharmaceuticals
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
11150177 43 Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.EBI University of Maryland
11101358 24 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.EBI Central Pharmaceutical Research Institute
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
10673103 55 Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.EBI AstraZeneca R&D Montréal
10617088 15 Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.EBI University of Louisville
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
10579842 91 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.EBI Synaptic Pharmaceutical Corporation
10579841 113 Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.EBI Synaptic Pharmaceutical Corporation
10509931 18 Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.EBI University of Arizona
10447942 9 A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.EBI TBA
9767649 24 N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.EBI Research Triangle Institute
1972964 40 Design and synthesis of highly potent and selective cyclic dynorphin A analogues.EBI University of Arizona
1681106 27 Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.EBI Pfizer Inc.
1652019 12 Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.EBI University of Washington
29400965 83 Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles.EBI Julius Maximilian University of W£rzburg
28499731 100 Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of?-opioid receptor antagonists.EBI Theravance Biopharma US, Inc
28825813 79 Highly Potent and Selective New Diphenethylamines Interacting with the?-Opioid Receptor: Synthesis, Pharmacology, and Structure-Activity Relationships.EBI University of Innsbruck
28817277 34 Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.EBI Pfizer Inc.
24719329 3 Inhibition of the ribonuclease H activity of HIV-1 reverse transcriptase by GSK5750 correlates with slow enzyme-inhibitor dissociation.BDB McGill University
23940047 7 Nicotinamide adenine dinucleotide-induced multimerization of the co-repressor CtBP1 relies on a switching tryptophan.BDB Oregon Health and Science University
27227314 79 Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands.BDB University of Washington
27439469 8 Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase.BDB Duquesne University
26686773 24 Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.BDB German Cancer Research Center (DKFZ)
25800132 6 Flavonoids: true or promiscuous inhibitors of enzyme? The case of deoxyxylulose phosphate reductoisomerase.BDB Universite de Strasbourg
24831513 35 Functionalization of ▀-Caryophyllene Generates Novel Polypharmacology in the Endocannabinoid System.BDB University of Bern , BŘhlstrasse 28, CH-3012 Bern, Switzerland.
1997328 39 Structural requirements for the binding of the pituitary adenylate-cyclase-activating peptide to receptors and adenylate-cyclase activation in pancreatic and neuronal membranes.BDB Université Libre de Bruxelles
16807364 18 Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs.BDB Queen's University
18434145 56 Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.BDB MethylGene Inc.
17602602 117 Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.BDB Research Triangle Institute
17154495 46 Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.BDB University of Southampton
17585750 63 Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.BDB Amgen
17336521 18 Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.BDB Yale University
16277992 12 Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S.BDB Georgia State University
2002466 13 Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.BDB Merck Sharp and Dohme Research Laboratories