Page last updated: 2024-08-07 16:37:31
Nociceptin receptor
A nociceptin receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P41146]
Synonyms
Kappa-type 3 opioid receptor;
KOR-3;
Orphanin FQ receptor
Research
Bioassay Publications (48)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (4.17) | 18.2507 |
2000's | 29 (60.42) | 29.6817 |
2010's | 15 (31.25) | 24.3611 |
2020's | 2 (4.17) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
j 113397 | Homo sapiens (human) | Kb | 0.0006 | 1 | 1 |
j 113397 | Homo sapiens (human) | Ke | 0.0008 | 1 | 1 |
sb-612111 | Homo sapiens (human) | Kb | 0.0018 | 3 | 3 |
nociceptin | Homo sapiens (human) | Kb | 0.0026 | 1 | 1 |
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
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 candJournal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Design and synthesis of novel small molecule N/OFQ receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
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).Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor.European journal of medicinal chemistry, , Volume: 46, Issue:4, 2011
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
[no title available]Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
Identification of an Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.Bioorganic & medicinal chemistry, , Apr-15, Volume: 22, Issue:8, 2014
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
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.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
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.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
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: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
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 aJournal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
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.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.Journal of medicinal chemistry, , Nov-21, Volume: 45, Issue:24, 2002
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Enables
This protein enables 4 target(s):
Target | Category | Definition |
nociceptin receptor activity | molecular function | Combining with the peptide nociceptin, and transmitting the signal across the membrane by activating an associated G-protein. [GOC:bf, GOC:mah, PMID:18670432] |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
Located In
This protein is located in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
cytoplasmic vesicle | cellular component | A vesicle found in the cytoplasm of a cell. [GOC:ai, GOC:mah, GOC:vesicles] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 15 target(s):
Target | Category | Definition |
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
sensory perception | biological process | The series of events required for an organism to receive a sensory stimulus, convert it to a molecular signal, and recognize and characterize the signal. This is a neurological process. [GOC:ai, GOC:dph] |
sensory perception of pain | biological process | The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators] |
response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
positive regulation of urine volume | biological process | Any process that increases the amount of urine excreted from the body over a unit of time. [GOC:mtg_25march11, GOC:yaf] |
G protein-coupled opioid receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by an opioid binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:bf, PMID:20494127] |
eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
negative regulation of cAMP-mediated signaling | biological process | Any process which stops, prevents, or reduces the frequency, rate or extent of cAMP-mediated signaling. [GOC:jl] |
estrous cycle | biological process | A type of ovulation cycle, which occurs in most mammalian therian females, where the endometrium is resorbed if pregnancy does not occur. [GOC:jl, Wikipedia:Estrous_cycle] |
negative regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio] |
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of an adenylate cyclase-activating G protein-coupled receptor signaling pathway. [GOC:hjd, PMID:19246489] |
regulation of locomotor rhythm | biological process | Any process that modulates the frequency, rate or extent of locomotor rhythm. [GO_REF:0000058, GOC:TermGenie, PMID:16310969] |
conditioned place preference | biological process | The associative learning process by which an animal learns and remembers an association between a neutral, unchanging environment and a putatively rewarding, internal state produced by a xenobiotic or drug. [PMID:21549821] |
neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |