The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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 |
| 27035422 |
46 |
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. |
Vrije Universiteit Brussel |
| 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 |
| 26390077 |
42 |
Tactical Approaches to Interconverting GPCR Agonists and Antagonists. |
University of Minnesota |
| 25284251 |
12 |
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor. |
Kyushu 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 |
| 25898137 |
61 |
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 |
| 25556095 |
32 |
A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety. |
West Chester University |
| 24973818 |
70 |
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists. |
University of Bath |
| 24761755 |
76 |
Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity. |
University of Bath |
| 24657054 |
66 |
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II. |
Astraea Therapeutics |
| 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 |
| 23582449 |
20 |
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 |
| 23466604 |
36 |
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
Universit£ |
| 23623415 |
33 |
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I. |
Astraea Therapeutics |
| 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 |
| 19473027 |
21 |
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists. |
National Institute of Neuroscienc |
| 17490886 |
7 |
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids. |
University of Ferrara |
| 21438532 |
13 |
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography. |
National Institute of Mental Health |
| 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 |
| 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 |
| 19879767 |
5 |
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation. |
Kyushu University |
| 19683449 |
116 |
Synthesis and pharmacological evaluation of 6-naltrexamine analogs for alcohol cessation. |
Human Biomolecular Research Institute |
| 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 |
| 18624395 |
16 |
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues. |
University of Maryland |
| 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 |
| 18068993 |
31 |
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist. |
Kyushu University |
| 17428659 |
192 |
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1. |
Schering-Plough Research Institute |
| 16814543 |
14 |
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 |
| 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 |
| 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 |
| 12431062 |
33 |
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist. |
Universit£ |
| 12431054 |
28 |
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints. |
Purdue Pharma |
| 11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
| 10753470 |
95 |
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor. |
F. Hoffmann-La Roche |
| 8021929 |
13 |
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety. |
University of Minnesota |
| 14980696 |
47 |
Design and synthesis of novel small molecule N/OFQ receptor antagonists. |
Purdue Pharma |
| 14684324 |
46 |
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands. |
Sri International |
| 12372523 |
134 |
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands. |
Schering-Plough Research Institute |
| 21866885 |
71 |
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine. |
University of Bath |
| 21330016 |
96 |
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor. |
Istituto Superiore Di Sanit£ |
| 20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
| 19818611 |
100 |
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach. |
Schering-Plough Research Institute |
| 19604695 |
49 |
Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure. |
Banyu Tsukuba Research Institute |
| 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 |
| 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 |
| 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 |
| 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 |
| 18448337 |
31 |
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability. |
Banyu Tsukuba Research Institute |
| 17420123 |
219 |
Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2. |
Schering-Plough Research Institute |
| 17289383 |
157 |
Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands. |
Schering-Plough Research Institute |
| 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 |
| 16876401 |
48 |
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
Jerini |
| 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 |
| 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 |
| 16621546 |
54 |
Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists. |
Banyu Tsukuba Research Institute |
| 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 |
| 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 |
| 16153834 |
102 |
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor. |
Johnson & Johnson Pharmaceutical Research and Development |
| 15664818 |
81 |
Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists. |
Organon Laboratories |
| 15454210 |
36 |
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. |
Purdue Pharma |
| 15225731 |
2 |
Synthesis and biological evaluation of the major metabolite of atomoxetine: elucidation of a partial kappa-opioid agonist effect. |
Johnson and Johnson Pharmaceutical |
| 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 |
| 15027881 |
32 |
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2. |
Vrije Universiteit Brussel |
| 12951102 |
46 |
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor. |
Purdue Pharma |
| 11689089 |
30 |
Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides. |
Tohoku Pharmaceutical University |
| 11101358 |
24 |
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. |
Central Pharmaceutical Research Institute |
| 27660683 |
36 |
Treatment of Pain with Spirocylic Cyclohexane Derivatives Having Dual Specificity for ORL-1 and ?-Opioid Receptors. |
Dart Neuroscience |
| 26878436 |
31 |
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility. |
Astraea Therapeutics |
| 30562697 |
84 |
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
University of Silesia In Katowice |
| 10602690 |
36 |
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397). |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
| 29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
| 31951130 |
107 |
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models. |
Astraea Therapeutics |
| 18249547 |
69 |
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties. |
Organon Laboratories |
| 15743186 |
41 |
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands. |
University of Ferrara |
| 12519064 |
48 |
Novel hexahydrospiro[piperidine-4,1'-pyrrolo[3,4-c]pyrroles]: highly selective small-molecule nociceptin/orphanin FQ receptor agonists. |
F. Hoffmann-La Roche |
| 11689082 |
29 |
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 |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 28776992 |
110 |
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. |
Northwestern University |
| 23940047 |
7 |
Nicotinamide adenine dinucleotide-induced multimerization of the co-repressor CtBP1 relies on a switching tryptophan. |
Oregon Health and Science University |
| 26686773 |
24 |
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity. |
German Cancer Research Center (Dkfz) |
| 9303561 |
3 |
Human serotonin 5-HT7 receptor: cloning and pharmacological characterisation of two receptor variants. |
Organon |
| 9298538 |
16 |
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b). |
Roche Bioscience |
| 9281594 |
12 |
Molecular cloning and pharmacological characterization of a new galanin receptor subtype. |
The Schering Plough Research Institute |
| 7774675 |
35 |
Characterisation of melanocortin receptor subtypes by radioligand binding analysis. |
Uppsala |
| 1997328 |
39 |
Structural requirements for the binding of the pituitary adenylate-cyclase-activating peptide to receptors and adenylate-cyclase activation in pancreatic and neuronal membranes. |
UniversitÉ |
| 17602602 |
117 |
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. |
Research Triangle Institute |
| 17585750 |
63 |
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. |
Amgen |
| 17336521 |
18 |
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains. |
Yale University |
| 15080999 |
10 |
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles. |
Wyeth Research |
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