436 articles for thisTarget
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Article Title
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Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective¿-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Dr. August Wolff Gmbh & Co. Kg Arzneimittel
Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.
West Virginia University School Of Pharmacy
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University Of Catania
Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies.
University Of Tsukuba
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
Synthesis, antinociceptive activity, and opioid receptor profiles of substituted trans-3-(decahydro- and octahydro-4a-isoquinolinyl)phenols.
Glaxo Group Research
Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.
University Of Minnesota
Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2.
TBA
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.
TBA
Stereochemical studies on medicinal agents. 25. Absolute configuration and analgetic potency of beta-1,2-dimethyl-2-phenyl-4-(propionyloxy)piperidine enantiomers.
TBA
Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics.
TBA
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
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University Of Kansas
Structural determinants of diphenethylamines for interaction with the¿ opioid receptor: Synthesis, pharmacology and molecular modeling studies.
University Of Innsbruck
The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
St. John'S University
Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacyµ-Opioid Receptor (MOR)/d-Opioid Receptor (DOR) Ligands.
University Of Michigan
Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans.
Ironwood Pharmaceuticals
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral¿-opioid receptor agonists.
China Pharmaceutical University
Discovery of Potent and Selective Agonists ofd Opioid Receptor by Revisiting the"Message-Address" Concept.
Fudan University
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
Evaluation of N-substituent structural variations in opioid receptor profile of LP1.
University Of Catania
Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.
Kitasato University
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University Of Minnesota
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.
University Of Michigan
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.
Medical University Of Lodz
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
Medical University Of Lodz
Multitarget opioid ligands in pain relief: New players in an old game.
University Of Catania
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacyµ-Opioid Receptor (MOR) Agonists/d-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
University Of Michigan
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
The University Of Kansas
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Mercachem
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.
Harvard Medical School
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
University Of Tsukuba
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.
Kitasato University
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
Synthesis and Pharmacology of a Novel¿ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.
Kitasato University
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.
Pharmacokinetics
Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.
Pharmacokinetics
Potency enhancement of the¿-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.
University Of Kansas Specialized Chemistry Center
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Medical University Of Lodz
C7ß-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.
University Of Bath
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
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
Universit£
Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists.
Dr. Reddy'S Laboratories
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
West Chester University
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
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
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.
Westf£Lische Wilhelms-Universit£T M£Nster
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University Of Bath
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.
The University Of Kansas
Synthesis and¿-opioid receptor activity of furan-substituted salvinorin A analogues.
The University Of Kansas
Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.
The University Of Mississippi
Synthesis of a novel universal opioid receptor agonist with the 1,3,5-trioxazatriquinane skeleton and its pharmacologies.
Kitasato University
Michael acceptor approach to the design of new salvinorin A-based high affinity ligands for the kappa-opioid receptor.
University Of Mississippi
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
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
Design and synthesis of quinolinopropellane derivatives with selectived opioid receptor agonism.
University Of Tsukuba
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.
University Of Bath
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Astraea Therapeutics
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
Kitasato University
Endomorphin analogues with mixedµ-opioid (MOP) receptor agonism/d-opioid (DOP) receptor antagonism and lackingß-arrestin2 recruitment activity.
Nanjing Medical University
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
Development of a bioavailableµ opioid receptor (MOPr) agonist,d opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.
University Of Michigan
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
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.
Lanzhou University
Opioid peptidomimetics: leads for the design of bioavailable mixed efficacyµ opioid receptor (MOR) agonist/d opioid receptor (DOR) antagonist ligands.
University Of Michigan
The effect of 17-N substituents on the activity of the opioid¿ receptor in nalfurafine derivatives.
Kitasato University
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Eli Lilly
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
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
National Institute Of Neuroscienc
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
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
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
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.
University Of Innsbruck
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
14-Alkoxy- and 14-acyloxypyridomorphinans:µ agonist/d antagonist opioid analgesics with diminished tolerance and dependence side effects.
Southern Research Institute
Opioid activity profiles of oversimplified peptides lacking in the protonable N-terminus.
University Of Bologna
cis-4-amino-L-proline residue as a scaffold for the synthesis of cyclic and linear endomorphin-2 analogues: part 2.
Universit£
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1.
The University Of Queensland
Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixedµ/d opioid receptor agonistic properties.
Vrije Universiteit Brussel
Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.
Harvard Medical School
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Kitasato University
Generation of novel radiolabeled opiates through site-selective iodination.
Memorial Sloan-Kettering Cancer Center
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
National Institute Of Mental Health
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
Opioid bifunctional ligands from morphine and the opioid pharmacophore Dmt-Tic.
University Of Cagliari
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
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
University Of Sydney
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
Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.
Kitasato University
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
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Wilhelms-Universit£T M£Nster
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute Of Montreal
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College And The Graduate Center Of The City University Of New York
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
Human Biomolecular Research Institute
Synthesis and opioid receptor activity of indolopropellanes.
Chinese Academy Of Sciences
Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Adolor
Syntheses of novel high affinity ligands for opioid receptors.
Rensselaer Polytechnic Institute
14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
Virginia Commonwealth University
Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.
Harvard Medical School
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
University Of Bath
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
Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
Virginia Commonwealth University
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
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Rensselaer Polytechnic Institute
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
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
Development of potent and selective small-molecule human Urotensin-II antagonists.
Glaxosmithkline
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Adolor
Herkinorin analogues with differential beta-arrestin-2 interactions.
The University Of Iowa
Synthesis and pharmacological evaluation of bicyclic SNC80 analogues with separated benzhydryl moiety.
Westf£Lische Wilhelms-Universit£T
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Harvard Medical School
Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Mclean Hospital
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Banyu Tsukuba Research Institute
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
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
3-Hydroxy-4-methoxyindolomorphinans as delta opioid selective ligands.
University Of Maryland
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Eli Lilly
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
University Of Bath
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
The University Of Iowa
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
High-affinity carbamate analogues of morphinan at opioid receptors.
Harvard Medical School
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Harvard Medical School
Effects of substitution on the pyrrole N atom in derivatives of tetrahydronaltrindole, tetrahydrooxymorphindole, and a related 4,5-epoxyphenylpyrrolomorphinan.
University Of Bath
Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu-opioid receptor antagonists.
Adolor
Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu-opioid receptor antagonists.
Adolor
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
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
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
University Of Bristol
Discovery of novel triazole-based opioid receptor antagonists.
University Of Medicine And Dentistry Of New Jersey And Umdnj Informatics Institute
A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.
Kaist
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Harvard Medical School
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore.
University Of Bath
Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone.
Rensselaer Polytechnic Institute
Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.
Harvard Medical School
Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2).
Mclean Hospital
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
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Harvard Medical School
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Abbott Laboratories
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.
University Of Innsbruck
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
University Of Bath
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
University Of Bath
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Harvard Medical School
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.
University Of Bath
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£
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
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
Structure-activity relationships of dynorphin a analogues modified in the address sequence.
University Of California
The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity.
Universit£
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.
TBA
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
Universit£
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
University Of Bristol
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).
University Of Minnesota
From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.
Universities Of Lille
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Research Triangle Institute
Structural determinants of opioid activity in the orvinols and related structures: ethers of orvinol and isoorvinol.
University Of Bristol
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
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Isosteric replacement of acidic with neutral residues in extracellular loop-2 of the kappa-opioid receptor does not affect dynorphin A(1-13) affinity and function.
University Of Minnesota
Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
University Of Minnesota
Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.
University Of Bristol
3-Deoxyclocinnamox: the first high-affinity, nonpeptide mu-opioid antagonist lacking a phenolic hydroxyl group.
University Of Bristol
[Pro(3)]Dyn A(1-11)-NH(2): a dynorphin analogue with high selectivity for the kappa opioid receptor.
University Of California
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.
University Of Minnesota
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
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
7-Spiroindanyl derivatives of naltrexone and oxymorphone as selective ligands for delta opioid receptors.
University Of Minnesota
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
14 alpha,14' beta-[Dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis (7,8-dihydromorphinone) and 14 alpha,14' beta-[dithiobis[(2-oxo-2,1- ethanediyl)imino]]bis[7,8-dihydro-N-(cyclopropylmethyl)normorphinone]: chemistry and opioid binding properties.
Institute
A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines.
Glaxo Group Research
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Oregon State University
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
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
University Of Washington
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
University Of Washington
Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.
Parke-Davis Research Unit
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Sri International
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Adolor
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
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
Synthesis of enantiomerically pure (+)- and (-)-18-methoxycoronaridine hydrochloride and their preliminary assessment as anti-addictive agents.
Albany Molecular Research
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
University Of Bristol
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.
Research Triangle Institute
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
Research Triangle Institute
A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine.
University Of Michigan
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
¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.
Astrazeneca R&D Montreal
Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.
Harvard Medical School
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
Institute Of Radiopharmacy
Discovery of aminobenzyloxyarylamides as¿ opioid receptor selective antagonists: application to preclinical development of a¿ opioid receptor antagonist receptor occupancy tracer.
Eli Lilly
Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.
University Of Illinois At Chicago
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University Of Bath
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University Of Sydney
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
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
Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens.
The University Of Mississippi
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
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
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.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.
Harvard Medical School
Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.
University Of Iowa
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Istituto Superiore Di Sanit£
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
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
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
Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.
University Of Mississippi
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
Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.
Harvard Medical School
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Astrazeneca Pharmaceuticals
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
Hokkaido University
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Astrazeneca Pharmaceuticals
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Purdue University
Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.
Griffith University
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Harvard Medical School
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Amgen
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
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Pfizer
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
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Pfizer
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.
Fudan University
Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.
Institute Of Chemical Biology
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
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Harvard Medical School
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
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO.
Biomedizinische Forschungsreagenzien
Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Harvard Medical School
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
14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
University Of Bristol
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
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
Pentapeptides displaying mu opioid receptor agonist and delta opioid receptor partial agonist/antagonist properties.
University Of Michigan
Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
University Of New England
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
Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Tsukuba Research Institute
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
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists
TBA
Synthesis and opioid binding properties of 2-chloroacrylamido derivatives of 7,8-dihydromorphinans
TBA
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)
TBA
N-Methyl and N-cyclopropylmethyl-14α,14′β-[dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydro-5β-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: Synthesis and opioid binding properties
TBA
Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective κ-opioid receptor agonists
TBA
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
Schering-Plough Research Institute
Discovery of mu-opioid selective ligands derived from 1-aminotetralin scaffolds made via metal-catalyzed ring-opening reactions.
University Of Toronto
Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Mclean Hospital
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
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
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.
Harvard Medical School
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
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Glaxosmithkline
Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
Tsukuba Research Institute
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Institut FüR Pharmazeutische Und Medizinische Chemie
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Banyu Tsukuba Research Institute
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
University Of Maryland
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A.
The University Of Iowa
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.
National Institute Of Mental Health
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.
Holden Laboratories
Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Eli Lilly
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
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
Pyrrolidino-tetrahydroisoquinolines bearing pendant heterocycles as potent dual H3 antagonist and serotonin transporter inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
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
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
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
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
Chinese Academy Of Sciences
In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Harvard Medical School
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Schering-Plough Research Institute
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
University Of Mississippi
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Schering-Plough Research Institute
Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.
Harvard Medical School
New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Harvard Medical School
Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Mclean Hospital
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.
Institute For Molecular Studies
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
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
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
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.
The University Of Iowa
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College Of Physicians And Surgeons
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Banyu Tsukuba Research Institute
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
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
Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor agonists.
Adolor
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Johnson And Johnson Pharmaceutical Research And Development
Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Adolor
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research And Development
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College Of Physicians And Surgeons
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
Harvard Medical School
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
The University Of Iowa
Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Adolor
Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists.
Adolor
Azepinone as a conformational constraint in the design of kappa-opioid receptor agonists.
Adolor
Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Johnson & Johnson Pharmaceutical Research & Development
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
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
Sri International
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
Vrije Universiteit Brussel
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Purdue Pharma
New scaffolds in the development of mu opioid-receptor ligands.
Astrazeneca R&D Montreal
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
Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Rensselaer Polytechnic Institute
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.
University Of Maryland
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
Shire Biochem
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.
University Of California
3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
Astrazeneca R&D MöLndal
Novel C-terminus modifications of the Dmt-Tic motif: a new class of dipeptide analogues showing altered pharmacological profiles toward the opioid receptors.
Astrazeneca R&D Montreal
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College Of Physicians And Surgeons
Stereospecific synthesis of (2S)-2-methyl-3-(2',6'-dimethyl-4'-hydroxyphenyl)-propionic acid (Mdp) and its incorporation into an opioid peptide.
Clinical Research Institute Of Montreal
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Central Pharmaceutical Research Institute
N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues.
Astrazeneca R&D Montreal
New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability.
Astrazeneca R&D Montreal
Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones.
University Of WüRzburg
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
Pfizer
Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.
Astrazeneca R&D MontréAl
Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.
University Of Illinois At Chicago
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.
TBA
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Research Triangle Institute
4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists.
Glaxo Group Research
14 beta-[(p-nitrocinnamoyl)amino]morphinones, 14 beta-[(p-nitrocinnamoyl)amino]-7,8-dihydromorphinones, and their codeinone analogues: synthesis and receptor activity.
Institute
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.
TBA
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
TBA
Design and synthesis of highly potent and selective cyclic dynorphin A analogues.
University Of Arizona
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues.
Eisai
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
University Of Washington
Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.
Harvard Medical School
New kappa-receptor agonists based upon a 2-[(alkylamino)methyl]piperidine nucleus.
Glaxo Group Research
Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands.
University Of Washington
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.
Broad Institute
Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase.
Duquesne University
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Emory University
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
Yogi Vemana University
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
German Cancer Research Center (Dkfz)
Flavonoids: true or promiscuous inhibitors of enzyme? The case of deoxyxylulose phosphate reductoisomerase.
University Of Strasburg
Ebselen Inhibits Hepatitis C Virus NS3 Helicase Binding to Nucleic Acid and Prevents Viral Replication
University Of Wisconsin-Milwaukee
N-formylpyrazolines and N-benzoylpyrazolines as novel inhibitors of mammalian cathepsin B and cathepsin H.
Kurukshetra University
A small molecule screen identifies selective inhibitors of urea transporter UT-A.
University Of California San Francisco
Substrate envelope-designed potent HIV-1 protease inhibitors to avoid drug resistance.
University Of Massachusetts
Novel synthesis of dihydropyrimidines for a-glucosidase inhibition to treat type 2 diabetes: in vitro biological evaluation and in silico docking.
Comsats Institute Of Information Technology
Structural requirements for the binding of the pituitary adenylate-cyclase-activating peptide to receptors and adenylate-cyclase activation in pancreatic and neuronal membranes.
UniversitÉ
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Research Triangle Institute
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Amgen
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
Yale University
Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
Ligand Pharmaceuticals
Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S.
Georgia State University
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70.
Ariad Pharmaceuticals
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
Merck Sharp And Dohme Research Laboratories