121 articles for thisTarget
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Article Title
Organization
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
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
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Vrije Universiteit Brussel
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
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
Kyushu 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
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
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.
West Chester University
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
University of Bath
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
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
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
Universit£
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
Astraea Therapeutics
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
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography.
National Institute of Mental Health
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
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
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
Kyushu University
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation.
Human Biomolecular Research Institute
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
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues.
University of Maryland
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
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
Kyushu University
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Schering-Plough Research Institute
Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide.
Tohoku Pharmaceutical University
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
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
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
Universit£
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
Purdue Pharma
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
F. Hoffmann-La Roche
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
University of Minnesota
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
Sri International
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Schering-Plough Research Institute
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
University of Bath
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.
Istituto Superiore Di Sanit£
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Schering-Plough Research Institute
Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure.
Banyu Tsukuba Research Institute
Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Tsukuba Research Institute
Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.
Schering-Plough 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
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
Structure-activity relationships of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the treatment of cough.
Schering-Plough Research Institute
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
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Banyu Tsukuba Research Institute
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Schering-Plough Research Institute
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Organon Laboratories
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.
Jerini
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
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
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
Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists.
Banyu Tsukuba Research Institute
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.
Banyu Tsukuba Research Institute
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
F. Hoffmann-La Roche
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.
F. Hoffmann-La Roche
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.
Organon Laboratories
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Purdue Pharma
Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect.
Johnson and Johnson Pharmaceutical
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
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.
Research Triangle Institute
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NH
University of Ferrara
Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides.
Tohoku Pharmaceutical University
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
Central Pharmaceutical Research Institute
Treatment of Pain with Spirocylic Cyclohexane Derivatives Having Dual Specificity for ORL-1 and ?-Opioid Receptors.
Dart Neuroscience
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
Astraea Therapeutics
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
University of Silesia In Katowice
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
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.
Astraea Therapeutics
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Organon Laboratories
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
University of Ferrara
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists.
F. Hoffmann-La Roche
Structure-activity studies of the Phe(4) residue of nociceptin(1-13)-NH(2): identification of highly potent agonists of the nociceptin/orphanin FQ receptor.
University of Ferrara
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Nicotinamide adenine dinucleotide-induced multimerization of the co-repressor CtBP1 relies on a switching tryptophan.
Oregon Health and Science University
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
German Cancer Research Center (Dkfz)
Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants.
Organon
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
Roche Bioscience
Molecular cloning and pharmacological characterization of a new galanin receptor subtype.
The Schering Plough Research Institute
Characterisation of melanocortin receptor subtypes by radioligand binding analysis.
Uppsala
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