438 articles for thisTarget

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The following articles (labelled with PubMed ID or TBD) are for your review

PMID	Data	Article Title	Organization
28318942	10	Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.	Medical University Of Lodz
28011222	16	Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.	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.	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.	National Health Research Institutes
1310115	11	Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols.	Glaxo Group Research
2475628	5	Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.	University Of Minnesota
2872334	16	Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.	TBA
3020245	4	Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.	TBA
6312042	7	Different receptor sites mediate opioid agonism and antagonism.	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.	TBA
6106064	20	Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.	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.	F. Hoffmann-La Roche
27876250	60	Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH	Jagiellonian University Medical College
27839919	192	Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.	University Of Kansas
27567368	12	Structural determinants of diphenethylamines for interaction with the¿ opioid receptor: Synthesis, pharmacology and molecular modeling studies.	University Of Innsbruck
27299736	37	The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.	St. John'S University
27096047	73	Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.	Fudan University
27035422	46	Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.	Vrije Universiteit Brussel
27079125	56	Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.	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.	Pfizer
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.	Jagiellonian University Medical College
26819673	55	Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.	Astrazeneca
26390077	42	Tactical Approaches to Interconverting GPCR Agonists and Antagonists.	University Of Minnesota
26944625	26	Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.	Medical University Of Lodz
26785295	35	Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.	Medical University Of Lodz
26656913	85	Multitarget opioid ligands in pain relief: New players in an old game.	University Of Catania
26739781	237	Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.	The Alexander Shulgin Research Institute
26789491	44	Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.	Torrey Pines Institute For Molecular Studies
26632862	20	Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting theµ-Opioid Receptor.	University Of Nottingham
26403932	9	Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.	Lanzhou University
26348881	54	Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.	National Health Research Institutes
26125201	62	Structural Requirements for CNS Active Opioid Glycopeptides.	The University Of Arizona
26048798	45	Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.	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.	Kitasato University
25147603	39	Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.	Pharmacokinetics
25147602	43	Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.	Pharmacokinetics
25593096	65	Potency enhancement of the¿-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.	University Of Kansas Specialized Chemistry Center
26005537	72	Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.	Medical University Of Lodz
25901762	33	Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of thed-opioid receptor.	Bristol-Myers Squibb
25494650	8	CNS drug design: balancing physicochemical properties for optimal brain exposure.	Eli Lilly
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.	National Institute On Drug Abuse
25783191	87	Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14ß-dihydroxy-4,5a-epoxy-6a-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.	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.	Novartis Pharma
25754490	44	trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.	Novartis Pharma
25513968	21	Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.	Universit£
25599839	75	Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.	Dr. Reddy'S Laboratories
25556095	32	A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.	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.	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.	National Health Research Institutes
25062506	102	Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.	Westf£Lische Wilhelms-Universit£T M£Nster
24973818	70	Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.	University Of Bath
24881566	140	Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).	Glaxosmithkline
25268943	116	Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.	The University Of Mississippi
25248680	67	Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.	Kitasato University
25193297	91	Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.	University Of Mississippi
24856182	23	Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.	Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
24933507	15	Synthesis and evaluation of three structurally related¹8F-labeled orvinols of different intrinsic activities: 6-O-[¹8F]fluoroethyl-diprenorphine ([¹8F]FDPN), 6-O-[¹8F]fluoroethyl-buprenorphine ([¹8F]FBPN), and 6-O-[¹8F]fluoroethyl-phenethyl-orvinol ([¹8F]FPEO).	University Of Oslo
24871036	13	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.	Astrazeneca
24835200	18	Design and synthesis of quinolinopropellane derivatives with selectived opioid receptor agonism.	University Of Tsukuba
24761755	76	Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.	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.	University Of Texas Southwestern Medical Center
24690494	92	Antagonists of the kappa opioid receptor.	The Scripps Research Institute
24657054	66	Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.	Astraea Therapeutics
24900842	71	Novel delta opioid receptor agonists with oxazatricyclodecane structure.	Kitasato University
24613457	64	Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.	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.	Eli Lilly
24332089	35	Imidazole-derived agonists for the neurotensin 1 receptor.	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.	Rensselaer Polytechnic Institute
23548164	1	Neoclerodanes as atypical opioid receptor ligands.	University Of Kansas
23477419	64	Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.	Lanzhou University
23360448	18	Development of¿ opioid receptor antagonists.	Research Triangle Institute
23281966	8	Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.	Astrazeneca
22541041	84	Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.	Eli 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.	University Of Ferrara
21193310	81	Tetrahydroquinoline derivatives as opioid receptor antagonists.	Glaxosmithkline
19473027	21	Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.	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.	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).	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).	The University Of Sydney
23134120	72	Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.	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.	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.	Vrije Universiteit Brussel
23016952	71	14-Alkoxy- and 14-acyloxypyridomorphinans:µ agonist/d antagonist opioid analgesics with diminished tolerance and dependence side effects.	Southern Research Institute
22995061	37	Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.	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.	Universit£
21354674	14	The many faces of the adamantyl group in drug design.	University Of Sydney
22724433	76	A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).	Lanzhou University
23022277	13	Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives.	The University Of Queensland
23017884	4	Formylated polyamines as peptidomimetics.	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.	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).	Janssen Research And Development
22680612	11	Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.	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.	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.	Pfizer
22439881	157	Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.	Harvard Medical School
24900459	53	NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with µ-Opioid Agonist Activity.	TBA
22542010	31	Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.	Amgen
22464684	85	Semisynthetic neoclerodanes as kappa opioid receptor probes.	The University Of Kansas
21621410	44	Generation of novel radiolabeled opiates through site-selective iodination.	Memorial Sloan-Kettering Cancer Center
21351746	116	Aminothiazolomorphinans with mixed¿ andµ opioid activity.	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.	National Institute Of Mental Health
21216504	19	Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.	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 rela	Pfizer
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.	Aska Pharmaceutical
20599386	46	Evaluation of N-substitution in 6,7-benzomorphan compounds.	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.	H. Lundbeck
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.	Research Triangle Institute
20441176	76	Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.	Wilhelms-Universit£T M£Nster
20218625	27	"Carba"-analogues of fentanyl are opioid receptor agonists.	Clinical Research Institute Of Montreal
19963380	38	Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.	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.	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).	Sepracor
19595591	37	Synthesis and opioid receptor activity of indolopropellanes.	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.	Adolor
19282177	106	Syntheses of novel high affinity ligands for opioid receptors.	Rensselaer Polytechnic Institute
19217280	34	14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.	Virginia Commonwealth University
19253983	37	14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.	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.	Pfizer
19199782	72	Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.	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).	Adolor
19027293	149	Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.	Rensselaer Polytechnic Institute
18637671	21	Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.	Toray Industries
18468907	64	Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.	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.	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.	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.	Adolor
18380425	90	Herkinorin analogues with differential beta-arrestin-2 interactions.	The University Of Iowa
18249546	11	Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.	Westf£Lische Wilhelms-Universit£T
18468891	59	Identification of novel benzimidazole series of potent and selective ORL1 antagonists.	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.	Abbott Laboratories
18243691	18	Potent, selective MCH-1 receptor antagonists.	Hoffmann-La Roche
18242987	75	In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.	Sepracor
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.	Institute
17980586	79	Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.	Eli Lilly
17887741	133	Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.	University Of Bath
17580847	67	Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.	The University Of Iowa
17428659	192	Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.	Schering-Plough Research Institute
17276685	70	High-affinity carbamate analogues of morphinan at opioid receptors.	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.	Harvard Medical School
15588100	68	Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.	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.	Adolor
17149859	215	Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.	Adolor
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.	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.	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.	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.	F. Hoffmann-La Roche
16821764	54	Discovery of novel triazole-based opioid receptor antagonists.	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.	Vrije Universiteit Brussels
16257206	18	Derivatives of tramadol for increased duration of effect.	Sepracor
16392810	100	Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.	Harvard Medical School
16198561	99	Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.	Novartis Institutes For Biomedical Research
16220969	219	Designed multiple ligands. An emerging drug discovery paradigm.	Organon Laboratories
15743177	43	Synthesis and biological evaluation of meperidine analogues at monoamine transporters.	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.	University Of Bath
15808478	18	Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.	Rensselaer Polytechnic Institute
15745801	5	Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.	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.	Purdue Pharma
15055988	49	2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.	Harvard Medical School
12672258	99	14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.	University Of Bath
12593647	49	2,6-Dimethyltyrosine analogues of a stereodiversified ligand library: highly potent, selective, non-peptidic mu opioid receptor agonists.	Harvard University
14640558	54	Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.	University Of Bath
14613319	93	Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.	Harvard Medical School
13678399	54	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.	University Of Arizona
12519069	60	The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.	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.	Universit£
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.	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.	Research Triangle Institute
12747782	79	Structure-activity relationships of dynorphin a analogues modified in the address sequence.	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.	Universit£
11906279	2	Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.	TBA
12431062	33	Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.	Universit£
11784158	28	4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.	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.	University Of Minnesota
11297446	3	Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).	University Of Minnesota
11585444	295	From hit to lead. Analyzing structure-profile relationships.	Universities Of Lille
11585443	137	From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.	Universities Of Lille
10794701	48	Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.	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.	University Of Minnesota
10753470	95	High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.	F. Hoffmann-La Roche
10669565	20	Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.	University Of Minnesota
10649968	28	Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.	University Of Bristol
10966754	9	3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.	University Of Bristol
10893307	26	[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.	University Of California
10891118	6	Enkephalin glycopeptide analogues produce analgesia with reduced dependence liability.	University Of Northern Colorado
10891107	3	Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.	University Of Minnesota
10229619	4	Emerging molecular approaches to pain therapy.	Abbott Laboratories
10508425	68	Mixture-based synthetic combinatorial libraries.	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.	University Of California San Diego
9301674	60	Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.	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.	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.	University Of Minnesota
8126697	30	Synthesis of naltrexone-derived delta-opioid antagonists. Role of conformation of the delta address moiety.	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.	Virginia Commonwealth University
1361580	25	N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.	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.	University Of Washington
1320121	48	Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.	University Of Washington
2153826	11	Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.	University Of Washington
2213824	20	Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.	Pfizer
2567782	50	Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.	Parke-Davis Research Unit
14980696	47	Design and synthesis of novel small molecule N/OFQ receptor antagonists.	Purdue Pharma
15203136	39	(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.	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.	Sri International
12643904	12	Synthesis and binding affinity of neuropeptide Y at opiate receptors.	University Of North Carolina At Wilmington
14643346	65	trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.	Adolor
12372523	134	Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.	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.	Niddk
11055333	21	Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.	University Of Bristol
10206545	40	Ring constrained analogues of the orvinols: the furanomorphides.	University Of Bristol
9873602	11	A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.	University Of Michigan
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22357342	8	SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives asµ opioid ligands.	Pfizer
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.	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.	Astrazeneca R&D Montreal
22197137	61	4-Piperidin-4-ylidenemethyl-benzamides asd-opioid receptor agonists for CNS indications: identifying clinical candidates.	Astrazeneca Pharmaceuticals
22136765	31	Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.	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.	Eli Lilly
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.	Vrije Universiteit Brussel
21866885	71	Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.	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.	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).	Pfizer
21667972	5	Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.	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.	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.	Pfizer
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.	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.	Harvard Medical School
21338114	27	Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.	University Of Iowa
21330016	96	Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.	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.	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.	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.	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.	University Of Mississippi
20980153	83	Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.	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.	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.	Astrazeneca Pharmaceuticals
20813948	63	Spiroindolones, a potent compound class for the treatment of malaria.	Swiss Tropical And Public Health Institute
20681583	7	Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.	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.	Astrazeneca Pharmaceuticals
20591666	66	A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.	Università
20426456	12	Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.	Griffith University
20144870	51	Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.	Harvard Medical School
20144865	18	Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.	Kyorin Pharmaceutical
20137933	218	Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.	Amgen
19818611	100	Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.	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.	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.	Nida
20015649	53	Biaryl piperidines as potent and selective delta opioid receptor ligands.	Pfizer
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.	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.	Solvay Pharma
19928862	120	Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.	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.	Astrazeneca R & D Montr£Al
19679474	8	Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.	Lanzhou University
19632840	43	Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.	Tsukuba Research Institute
19694469	3	Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.	Biomedizinische Forschungsreagenzien
19634902	55	Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.	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.	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.	The University Of Kansas
19842669	34	14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.	University Of Bristol
19836950	9	Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.	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.	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.	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.	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).	Adolor
19564110	31	Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.	Tsukuba Research Institute
19678644	52	Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.	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.	Tsukuba Research Institute
8496700	16	The Role of Receptor Binding in Drug Discovery	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.	TBA
	8	The design and synthesis of kappa opioid ligands based on a binding model for kappa agonists	TBA
19339177	127	The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.	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.	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.	Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz
19231185	44	2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.	Pfizer
19168350	58	Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.	University Of Toronto
19113864	27	Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.	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.	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.	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.	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.	National Institute Of Mental Health
18701276	97	Highly functionalized 7-azaindoles as selective PPAR gamma modulators.	Merck Research Laboratories
18674902	48	Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.	Harvard Medical School
18640038	74	Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.	Amgen
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.	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.	Tsukuba Research Institute
18499305	11	1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.	Institut FüR Pharmazeutische Und Medizinische Chemie
18468445	26	Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides.	University Of Queensland
18448337	31	Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.	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.	University Of Queensland
17988766	26	Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.	University Of Maryland
16792410	48	Synthesis of salvinorin A analogues as opioid receptor probes.	The University Of Iowa
18207400	17	Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.	Medical University Of Lodz
17826995	48	Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.	Kobe Gakuin University
17826993	17	5'-halogenated analogs of oxymorphindole.	University Of Maryland
17720493	93	Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.	Eli Lilly
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.	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.	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.	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.	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.	Johnson & Johnson Pharmaceutical Research & Development
17488103	56	Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.	Chinese Academy Of Sciences
17433695	54	In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.	Harvard Medical School
17420123	219	Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.	Schering-Plough Research Institute
17350835	88	Further studies of tyrosine surrogates in opioid receptor peptide ligands.	Adolor
17289383	157	Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.	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).	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.	Organon Laboratories
16942040	12	New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.	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.	F. Hoffmann-La Roche
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.	F. Hoffmann-La Roche
16722655	28	Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.	Pfizer
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.	Predix Pharmaceuticals
16632355	116	3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.	Johnson & Johnson Pharmaceutical Research And Development
16621556	12	Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.	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.	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.	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.	F. Hoffmann-La Roche
16302812	6	Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents.	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.	Adolor
16275086	18	Synthesis and biological activity of the first cyclic biphalin analogues.	University Of Arizona
16263278	46	Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.	Adolor
16246561	90	Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.	F. Hoffmann-La Roche
16246557	75	Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.	F. Hoffmann-La Roche
16236510	85	4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.	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.	Adolor
16153834	102	Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.	Johnson & Johnson Pharmaceutical Research And Development
16143528	213	Synthesis of potent and selective serotonin 5-HT1B receptor ligands.	Columbia University College Of Physicians And Surgeons
16033256	57	Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.	The University Of Iowa
15863335	111	Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.	Adolor
15664818	81	Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.	Organon Laboratories
15482950	17	Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.	Adolor
15454210	36	Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.	Purdue Pharma
15163203	45	Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.	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.	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.	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.	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.	Instituto De QuíMica MéDica
12951102	46	Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.	Purdue Pharma
12699761	85	New scaffolds in the development of mu opioid-receptor ligands.	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.	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.	Astrazeneca R&D
12593663	146	Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.	Rensselaer Polytechnic Institute
12477343	8	Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.	University Of Maryland
12372519	22	Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.	Shire Biochem
12166947	30	Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.	University Of California
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