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284 articles for thisTarget


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PMIDDataArticle TitleOrganization
28218838 69 Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.EBI Dr. August Wolff Gmbh & Co. Kg Arzneimittel
28011222 16 Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.EBI West Virginia University School of Pharmacy
27721146 22 (+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/sEBI University of Catania
27676089 35 A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.EBI Clinical Research Institute of Montreal
27301366 30 [Dmt(1)]DALDA analogues modified with tyrosine analogues at position 1.EBI Nanjing Medical 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
26713106 59 Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.EBI Vrije Universiteit Brussel
26656913 85 Multitarget opioid ligands in pain relief: New players in an old game.EBI University of Catania
26712115 36 Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.EBI University of Arizona
26411794 46 Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.EBI Mercachem
26323872 49 Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.EBI University of Arizona
26299827 43 Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.EBI University of Arizona
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
25129170 20 'Carba'-carfentanil (trans isomer): aµ opioid receptor (MOR) partial agonist with a distinct binding mode.EBI Clinical Research Institute of Montreal
25544687 60 Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.EBI Vrije Universiteit Brussel
24973818 70 Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.EBI University of Bath
25221662 24 Novel cyclic biphalin analogue with improved antinociceptive properties.EBI Universit£
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
24839540 26 In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated DmtEBI Vrije Universiteit Brussel
24613457 64 Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.EBI Nanjing Medical University
24602401 40 [Dmt(1)]DALDA analogues with enhancedµ opioid agonist potency and with a mixedµ/¿ opioid activity profile.EBI Nanjing Medical University
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
23547584 19 Biological active analogues of the opioid peptide biphalin: mixeda/ß(3)-peptides.EBI Universit£
23360448 18 Development of¿ opioid receptor antagonists.EBI Research Triangle Institute
16290934 51 Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1.EBI Pfizer
11133082 32 Assessment of substitution in the second pharmacophore of Dmt-Tic analogues.EBI University of Naples
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
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
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£
22724433 76 A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).EBI Lanzhou University
22394120 7 The cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues.EBI Universit£
21641798 16 Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.EBI Kitasato University
21128594 93 Development of potent µ and d opioid agonists with high lipophilicity.EBI University of Arizona
20547453 122 Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.EBI University of Arizona
20218625 27 "Carba"-analogues of fentanyl are opioid receptor agonists.EBI Clinical Research Institute of Montreal
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
20560643 71 Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.EBI University of Arizona
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
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
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
18370374 12 Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.EBI Vrije Universiteit Brussel
18311909 10 Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.EBI Stanford University School of Medicine
18178091 24 Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).EBI University of Ferrara
17420073 31 Synthesis of bridged piperazines with sigma receptor affinity.EBI Institut F£R Pharmazeutische Und Medizinische Chemie
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
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
16942034 19 Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.EBI University of Cagliari
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
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
16509592 101 Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.EBI University of Arizona
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 Sapienza University of Rome
15863299 8 Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers.EBI University of Arizona
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
13678399 54 Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.EBI University of Arizona
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£
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
12459023 46 Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.EBI University of Cagliari
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
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
10794701 48 Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.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
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
9857089 32 Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.EBI Research Triangle Institute
9057861 33 (E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.EBI University of Washington
9057856 53 Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid rEBI National Institute of Diabetes and Digestive and Kidney Diseases
9301674 60 Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.EBI University of Ferrara
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
8831778 22 The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid receptoEBI University of Arizona
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
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
8164255 23 Cyclic beta-casomorphin analogues with mixed mu agonist/delta antagonist properties: synthesis, pharmacological characterization, and conformational aspects.EBI Clinical Research Institute of Montreal
7996538 42 Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.EBI University of Washington
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
8035418 30 Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.EBI National Institute of Diabetes and Digestive and Kidney Diseases
8021929 13 Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.EBI University of Minnesota
8021915 16 Newly discovered stereochemical requirements in the side-chain conformation of delta opioid agonists for recognizing opioid delta receptors.EBI University of Arizona
8201592 27 [L-Ala3]DPDPE: a new enkephalin analog with a unique opioid receptor activity profile. Further evidence of delta-opioid receptor multiplicity.EBI University of Arizona
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
8289188 30 Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.EBI University of Arizona
8246236 6 Possible contribution of a glutathione conjugate to the long-duration action of beta-funaltrexamine.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
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 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
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 29 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
1320121 48 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
1648137 30 Topographically designed analogues of [D-Pen,D-Pen5]enkephalin.EBI University of Arizona
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 23 Role of spacer and address components in peptidomimetic delta opioid receptor antagonists related to naltrindole.EBI University of Minnesota
1851843 96 Synthesis and structure-activity relationships of deltorphin analogues.EBI University of Ferrara
1849995 12 Role of the spacer in conferring kappa opioid receptor selectivity to bivalent ligands related to norbinaltorphimine.EBI University of Minnesota
1846919 26 Highly selective kappa opioid analgesics. 4. Synthesis of some conformationally restricted naphthalene derivatives with high receptor affinity and selectivity.EBI Parke-Davis Research Unit
2160538 84 Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.EBI University of Minnesota
2542556 65 Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.EBI Ciba-Geigy
2832603 68 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
2828622 71 Investigation of the structural parameters involved in the mu and delta opioid receptor discrimination of linear enkephalin-related peptides.EBI University of Paris
2887656 48 Synthesis and activity profiles of new dermorphin-(1-4) peptide analogues.EBI TBA
2444704 14 Hybrid bivalent ligands with opiate and enkephalin pharmacophores.EBI University of Minnesota
2879914 30 Peptides as receptor selectivity modulators of opiate pharmacophores.EBI TBA
2409281 9 10-Ketonaltrexone and 10-ketooxymorphone.EBI TBA
6296388 68 Synthesis and pharmacological characterization in vitro of cyclic enkephalin analogues: effect of conformational constraints on opiate receptor selectivity.EBI TBA
7154002 8 Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides.EBI TBA
6276540 20 Evidence of the preferential involvement of mu receptors in analgesia using enkephalins highly selective for peripheral mu or delta receptors.EBI TBA
15115401 24 Oral bioavailability of a new class of micro-opioid receptor agonists containing 3,6-bis[Dmt-NH(CH(2))(n)]-2(1H)-pyrazinone with central-mediated analgesia.EBI National Institutes of Environmental Health Sciences
12565965 45 Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.EBI Southern Research Institute
11755357 14 Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.EBI University of Louisville
11294396 57 Selective delta-opioid receptor ligands: potential PET ligands based on naltrindole.EBI University of Bristol
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
11055333 21 Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.EBI University of Bristol
10673107 63 8-Aminocyclazocine analogues: synthesis and structure-activity relationships.EBI Institute
10206545 40 Ring constrained analogues of the orvinols: the furanomorphides.EBI University of Bristol
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
9873603 23 Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.EBI University of Michigan
9873602 11 A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.EBI University of Michigan
 9 Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodimeEBI TBA
 21 Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogsEBI TBA
21967807 36 Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.EBI University of Pavia
21925887 10 Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.EBI University of Arizona
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
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
21366266 66 Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.EBI University of Arizona
21256034 58 Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.EBI Kitasato University
20692738 34 Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2.EBI Sapienza University of Rome
20685120 20 Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.EBI Kitasato University
20637637 46 Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds.EBI University of Cagliari
20617791 70 Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.EBI University of Arizona
20483601 22 Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.EBI Kitasato University
20476738 14 Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.EBI Universit£
20137938 28 Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.EBI Vrije Universiteit Brussel
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
19762245 69 The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.EBI University of Arizona
19540763 4 Synthesis and investigations of double-pharmacophore ligands for treatment of chronic and neuropathic pain.EBI University of Arizona
19621878 19 Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.EBI The University of Kansas
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
19642675 60 Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.EBI University of Cagliari
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
19560919 28 Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue.EBI Universit£
 12 The stereochemical requirements of the novel δ-opioid selective dipeptide antagonist TMT-TicEBI 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
 24 Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonistsEBI 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 Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin IEBI TBA
19062273 41 Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.EBI Vrije Universiteit Brussel
18821747 45 The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.EBI University of Arizona
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
17851080 6 A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.EBI University of Ferrara
17826995 48 Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.EBI Kobe Gakuin University
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
17339114 27 Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore.EBI University of Cagliari
17329100 34 Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.EBI University of Arizona
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
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
17201419 93 Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.EBI University of Arizona
17188879 16 Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.EBI Lanzhou University
17142049 40 Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.EBI Kobe Gakuin University
16949282 12 Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.EBI Kobe Gakuin University
16828552 20 Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.EBI University of Arizona
16759107 18 6-N,N-dimethylamino-2,3-naphthalimide: a new environment-sensitive fluorescent probe in delta- and mu-selective opioid peptides.EBI Universidad De Santiago De Compostela
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
16483774 66 Identification of potent phenyl imidazoles as opioid receptor agonists.EBI Johnson & Johnson Pharmaceutical Research & Development
16366592 33 Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).EBI University of Cagliari
16335927 48 Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.EBI Kobe Gakuin University
16275086 18 Synthesis and biological activity of the first cyclic biphalin analogues.EBI University of Arizona
16183273 12 New series of potent delta-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif.EBI Kobe Gakuin University
16107162 10 From the potent and selective mu opioid receptor agonist H-Dmt-d-Arg-Phe-Lys-NH(2) to the potent delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH.EBI University of Cagliari
15780619 15 Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.EBI Lanzhou University
15664820 1 Studies on the structure-activity relationship of 2',6'-dimethyl-l-tyrosine (Dmt) derivatives: bioactivity profile of H-Dmt-NH-CH(3).EBI Kobe Gakuin University
15658871 28 Development of potent mu-opioid receptor ligands using unique tyrosine analogues of endomorphin-2.EBI Kobe Gakuin University
15588089 10 Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.EBI University of Cagliary
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
15267245 10 Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.EBI University of Cagliary
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
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
12852751 34 Unique high-affinity synthetic mu-opioid receptor agonists with central- and systemic-mediated analgesia.EBI Kobe Gakuin University
12749896 47 Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.EBI Rensselaer Polytechnic Institute
12657261 32 Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.EBI Tohoku Pharmaceutical University
12593663 146 Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.EBI Rensselaer Polytechnic Institute
12166947 30 Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.EBI University of California
11958984 24 Dermorphin and deltorphin heptapeptide analogues: replacement of Phe residue by Dmp greatly improves opioid receptor affinity and selectivity.EBI Tohoku Pharmaceutical University
11755345 45 Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.EBI Niddk
11266156 42 8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.EBI Rensselaer Polytechnic Institute
11212102 24 Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.EBI Tohoku Pharmaceutical University
10753473 14 Deltorphin II analogues with 6-hydroxy-2-aminotetralin-2-carboxylic acid in position 1.EBI Hungarian Academy of Sciences
10639279 26 Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand.EBI The University of Arizona
10617088 15 Synthesis and biological activities of position one and three transposed analogs of the opioid peptide YKFA.EBI University of Louisville
31550662 109 Progress in the development of more effective and safer analgesics for pain management.EBI University of Catania
30939014 143 Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.EBI Universit£T M£Nster
30924650 73 Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic ?-Opioid Receptor (MOR) Agonist/?-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.EBI University of Michigan
30543421 74 Development of Novel Quinoxaline-Based ?-Opioid Receptor Agonists for the Treatment of Neuroinflammation.EBI Universit£T M£Nster
9873693 24 N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines are opioid receptor pure antagonists.EBI Research Triangle Institute
9873439 18 C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.EBI National Taiwan University
9871617 24 Modifications of the 4,4'-residues and SAR studies of Biphalin, a highly potent opioid receptor active peptide.EBI University of Arizona
9822547 41 De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the delta-opioid receptor.EBI The University of Arizona
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
9258365 28 Helix-inducing alpha-aminoisobutyric acid in opioid mimetic deltorphin C analogues.EBI National Institute of Environmental Health Sciences
9111295 48 Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the"address" sequence.EBI Oregon State University
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
26611918 45 Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.EBI University of Arizona
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
8576920 34 Design and synthesis of 1-aminocycloalkane-1-carboxylic acid-substituted deltorphin analogues: unique delta and mu opioid activity in modified peptides.EBI University of Ferrara
26465170 87 Discovery of Novel Multifunctional Ligands with ?/? Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.EBI University of Arizona
26212775 77 Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.EBI University of Arizona
8384662 20 A topochemical approach to explain morphiceptin bioactivity.EBI University of California
8289187 47 Design of cyclic deltorphins and dermenkephalins with a disulfide bridge leads to analogues with high selectivity for delta-opioid receptors.EBI University of Arizona
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
24220171 5 Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration.EBI Medical University of Lodz
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 Eli Lilly
23932788 60 N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.EBI Clinical Research Institute of Montreal
7996550 12 Development of a model for the delta opioid receptor pharmacophore. 2. Conformationally restricted Phe3 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).EBI University of Michigan
7996549 40 Development of a model for the delta opioid receptor pharmacophore. 1. Conformationally restricted Tyr1 replacements in the cyclic delta receptor selective tetrapeptide Tyr-c[D-Cys-Phe-D-Pen]OH (JOM-13).EBI University of Michigan
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
24648867 58 Chiral Effect of a Phe Residue in Position 3 of the DmtEBI University of Arizona
23822516 142 Cyclic enkephalins with a diversely substituted guanidine bridge or a thiourea bridge: synthesis, biological and structural evaluations.EBI Universit£
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
23517479 13 Orally active opioid compounds from a non-poppy source.EBI Temple University
23623418 140 Effect of anchoring 4-anilidopiperidines to opioid peptides.EBI University of Arizona
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
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
17555306 6 o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.EBI University of Minnesota
6313921 10 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
11960505 18 Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands.EBI Chiba University
29107424 27 Selective kappa opioid antagonists for treatment of addiction, are we there yet?EBI University of Science and Technology
29477074 79 Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review.EBI University of Catania
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
30350997 111 Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.EBI Universit£T M£Nster
2822930 48 Structure-activity relationships of cyclic opioid peptide analogues containing a phenylalanine residue in the 3-position.EBI Clinical Research Institute of Montreal
29152051 40 ?-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.EBI Vrije Universiteit Brussel
29853330 106 Chemical space screening around PheEBI Vrije Universiteit Brussel
28734666 23 Development of novel LP1-based analogues with enhanced delta opioid receptor profile.EBI University of Catania
1972964 40 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
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
1846921 56 (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.EBI Zambeletti Research Laboratories
1652025 45 (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
1331451 68 Conformationally restricted deltorphin analogues.EBI Clinical Research Institute of Montreal
28291693 1 Synthesis and evaluation of a ligand targeting the? and? opioid receptors for drug delivery to lung cancer.EBI Purdue University
26496515 11 Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling.BDB Quaid-I-Azam University
26520885 21 Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.BDB Hazara University