Page last updated: 2024-11-12

nociceptin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID16131448
CHEMBL ID396460
CHEBI ID80266
MeSH IDM0252734

Synonyms (35)

Synonym
170713-75-4
nociceptin (1-17)
human nociceptin
unii-7ayi9n34ff
7ayi9n34ff ,
nociceptin (human)
gtpl1681
orphanin fq (pig)
orphanin fq (human)
l-glutamine, l-phenylalanylglycylglycyl-l-phenylalanyl-l-threonylglycyl-l-alanyl-l-arginyl-l-lysyl-l-seryl-l-alanyl-l-arginyl-l-lysyl-l-leucyl-l-alanyl-l-asparaginyl-
orphanin fq (swine)
orphanin fq (rat)
orphanin fq
nociceptin ,
NCGC00167266-01
chebi:80266 ,
CHEMBL396460
nociceptin/orphanin fq
bdbm50004178
n-ofq peptide
nociceptin-orphanin fq
Y-100028
phe-gly-gly-phe-thr-gly-ala-arg-lys-ser-unk-ala-arg-lys-leu-ala-asn-gln
nociceptin [mi]
AKOS024458690
l-phenylalanylglycylglycyl-l-phenylalanyl-l-threonylglycyl-l-alanyl-l-arginyl-l-lysyl-l-seryl-l-alanyl-l-arginyl-l-lysyl-l-leucyl-l-alanyl-l-asparaginyl-l-glutamine
l-phe-gly-gly-l-phe-l-thr-gly-l-ala-l-arg-l-lys-l-ser-l-ala-l-arg-l-lys-l-leu-l-ala-l-asn-l-gln
fggftgarksarklanq
pheglyglyphethrglyalaarglysseralaarglysleualaasngln
Q4327722
c79h129n27o22
HB2424
orphanin-fq
orphanin fqorphanin fq
DTXSID60168933

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Our results in nonhuman primates suggest that bifunctional NOP/MOP agonists with the appropriate balance of NOP and MOP agonist activity may provide a dual therapeutic action for safe and effective pain relief and treating prescription opioid abuse."( A bifunctional nociceptin and mu opioid receptor agonist is analgesic without opioid side effects in nonhuman primates.
Czoty, PW; Daga, PR; Ding, H; Kiguchi, N; Kishioka, S; Ko, MC; Lu, JJ; Polgar, WE; Yasuda, D; Zaveri, NT, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
" These molecules also exhibit superior pharmacological and pharmacokinetic parameters, relative to all GlyT1 inhibitors of the spiropiperidine family, culminating in the identification of 16b with an oral bioavailability of approximately 60%."( 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.
Alberati, D; Hainzl, D; Jolidon, S; Kurt, A; Pinard, E; Thomas, AW; Zimmerli, D, 2006
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
" NST and NCP were isolated from human brain and CSF samples by affinity chromatography combined with HPLC."( Identification of mature nocistatin and nociceptin in human brain and cerebrospinal fluid by mass spectrometry combined with affinity chromatography and HPLC.
Chin, YC; Jikuya, H; Joseph, T; Kimura, T; Lee, TL; Ning, C; Nishiuchi, Y; Ou, K; Tachibana, S, 2006
)
0.33
" Thus, this study was purposed to investigate the molecular mechanism of OFQ combined with ADM that reverses multi-drug resistance of K562/ADM, as well as its correlation with the expression of MDR1 mRNA and P-glycoprotein (P-gp)."( [Orphanin FQ combined with adriamycin reverses multi-drug resistance of K562/ADM and its molecular mechanism].
Chen, X; Liu, XQ; Wang, XX; Zhang, W; Zhao, L, 2012
)
0.38
" In SD rats, a low, but not a high, dose of SAM in combination with BUP counteracted swim-stress induced immobility."( Locomotor and anti-immobility effects of buprenorphine in combination with the opioid receptor modulator samidorphan in rats.
Burke, NN; Deaver, DR; Ferdousi, M; Finn, DP; Kelly, JP; Roche, M, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" The main reasons for the higher bioavailability of the PNA-peptide conjugate were found to be a more rapid cellular uptake in combination with a lowered re-export and resistance against influences of serum."( Enhancement of intracellular concentration and biological activity of PNA after conjugation with a cell-penetrating synthetic model peptide.
Berger, H; Bienert, M; Ehrlich, A; Oehlke, J; Wallukat, G; Wiesner, B; Wolf, Y, 2004
)
0.32
" These molecules also exhibit superior pharmacological and pharmacokinetic parameters, relative to all GlyT1 inhibitors of the spiropiperidine family, culminating in the identification of 16b with an oral bioavailability of approximately 60%."( 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.
Alberati, D; Hainzl, D; Jolidon, S; Kurt, A; Pinard, E; Thomas, AW; Zimmerli, D, 2006
)
0.33
" Moreover, these compounds exhibit sufficient bioavailability to produce a high level of NOP receptor occupancy in the brain following oral administration in rats."( 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.
Barth, VN; Benito, A; Diaz, N; Jiménez, A; Joshi, EM; Kahl, SD; Lafuente, C; Martinez-Grau, MA; Mateos, C; McKinzie, D; Mudra, DR; Pedregal, C; Rash, KS; Shaw, DB; Statnick, MA; Toledo, MA; Torrado, A; Witkin, JM, 2014
)
0.4
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

Nociceptin (10 nmolxL(-1) enhanced buprenorphine anti-nociception. Cebranopadol caused rightward shifts of the antinociceptive dose-response curve.

ExcerptRelevanceReference
"5 nmol/h) of the agonist for 5 days, the OFQ dose-response curves for its antinociceptive effect in the tail-flick and paw-pressure tests were significantly shifted to the right."( Antinociceptive and morphine modulatory actions of spinal orphanin FQ.
Henderson, G; Jhamandas, KH; Sutak, M, 1998
)
0.3
" When wide ranges of N/OFQ doses were used, a typical bell-shaped dose-response relationship was observed in both peripheral and central nociception tests."( Dose-related opposite modulation by nociceptin/orphanin FQ of substance P nociception in the nociceptors and spinal cord.
Inoue, M; Sakurada, T; Shimohira, I; Takeshima, H; Ueda, H; Yoshida, A; Zimmer, A, 1999
)
0.3
" Both shifted the dose-response curve of morphine to the right and these actions were eliminated by intrathecal PGD(2."( Antianalgesic action of nociceptin originating in the brain is mediated by spinal prostaglandin E(2) in mice.
Campbell, WB; Fujimoto, JM; Rady, JJ, 2001
)
0.31
" Relative to morphine-naive control mice, significant rightward shifts in the morphine dose-response curve, resulting in increased morphine ED(50) values (approximately two to three-fold), was observed for all genotypes following three days of repeated systemic morphine injections."( Morphine tolerance and dependence in nociceptin/orphanin FQ transgenic knock-out mice.
Chen, ZP; Hopkins, E; Kest, B; Mogil, JS; Palmese, CA; Pintar, JE, 2001
)
0.31
" Dose-response curves for buprenorphine-induced antinociception display ceiling effects or are bell shaped, which have been attributed to the partial agonist activity of buprenorphine at opioid receptors."( Buprenorphine-induced antinociception is mediated by mu-opioid receptors and compromised by concomitant activation of opioid receptor-like receptors.
Bryant, CD; Carroll, FI; Eitan, S; Evans, CJ; Kieffer, BL; Lutfy, K; Maidment, NT; Saliminejad, N; Takeshima, H; Walwyn, W; Yang, YC, 2003
)
0.32
" Next, the dose-response effect of intra-VTA or intranigral OFQ/N (3 microg or 30 microg/0."( Orphanin FQ/nociceptin suppresses motor activity through an action along the mesoaccumbens axis in rats.
Carroll, FI; Lam, H; Lutfy, K; Narayanan, S, 2004
)
0.32
" Subsequent dose-response studies showed that OFQ/N suppressed motor activity even at a 10-fold-lower dose after intrategmental but not intranigral administration."( Orphanin FQ/nociceptin suppresses motor activity through an action along the mesoaccumbens axis in rats.
Carroll, FI; Lam, H; Lutfy, K; Narayanan, S, 2004
)
0.32
" In dose-response studies, Ro64-6198 increased [(35)S]-GTPgammaS binding to a variety of brain regions with EC(50) values ranging from 84."( Distribution of nociceptin and Ro64-6198 activated [35S]-GTPgammaS binding in the rat brain.
Gackenheimer, SL; Gehlert, DR; Shaw, JL, 2006
)
0.33
" These results indicate that the endogenous OFQ/N system is differentially involved in morphine tolerance development and establishment of opiate dependence, depending on the specific morphine dosage regimen."( Endogenous orphanin FQ/nociceptin is involved in the development of morphine tolerance.
Chung, S; Civelli, O; Pohl, S; Reinscheid, RK; Zeng, J, 2006
)
0.33
"0 nmol) administered concurrently into the BLA potentiated the dose-response effects of OFQ/N."( Orphanin FQ/nociceptin interacts with the basolateral amygdala noradrenergic system in memory consolidation.
Civelli, O; Lengvilas, R; McGaugh, JL; Reinscheid, RK; Roozendaal, B,
)
0.13
" Dose-response and time course curves were done."( Role of nociceptin/orphanin FQ and the pseudopeptide [Phe1Psi(CH2NH)Gly2]-nociceptin(1-13)-NH2 and their interaction with classic opioids in the modulation of thermonociception in the land snail Helix aspersa.
Cruz, SL; León-Olea, M; Miller-Pérez, C; Pellicer, F; Rodríguez-Manzo, G; Sánchez-Islas, E, 2008
)
0.35
") enhanced the ascending (3 mgxkg(-1)) and descending (30 mgxkg(-1)) portions of buprenorphine's dose-response curve, but only spinal, not supraspinal, nociceptin (10 nmolxL(-1)) enhanced buprenorphine anti-nociception."( Identification of an additional supraspinal component to the analgesic mechanism of action of buprenorphine.
Ding, Z; Raffa, RB, 2009
)
0.35
" The IC(50) value of SB-612111 estimated from dose-response curves is 87."( Quantitative study of the antagonistic effect of (-)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) on nociceptin/orphanin FQ-mediated potassium channel activation in rat periaqueducta
Chiou, LC; Jiang, F; Liao, YY, 2011
)
0.37
"03 mg/kg) produced similar degrees of rightward shifts of buprenorphine's dose-response curves for all three endpoints."( Roles of μ-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates.
Cremeans, CM; Gruley, E; Ko, MC; Kyle, DJ, 2012
)
0.38
" In these animal models, the dose-response curve for LPS was too steep to allow use in survival studies and no changes in the N/OFQ system occurred within 24h."( Exploring LPS-induced sepsis in rats and mice as a model to study potential protective effects of the nociceptin/orphanin FQ system.
Bath, MF; Lambert, DG; Stover, CM; Thomas, RC; Thompson, JP, 2014
)
0.4
" Pretreatment with antagonists selective for nociceptin and μ receptors, but not δ and κ receptor antagonists, caused rightward shifts of the antinociceptive dose-response curve of cebranopadol with dose ratios of 2 and 9, respectively."( Functional Profile of Systemic and Intrathecal Cebranopadol in Nonhuman Primates.
Caló, G; Ding, H; Hsu, FC; Kiguchi, N; Ko, MC; Trapella, C, 2021
)
0.62
" SCH221510 (3 mg/kg, sc) attenuated but SB612111 (10 mg/kg, sc) enhanced morphine-induced antinociception, with rightward and leftward shift of morphine dose-response curves, respectively."( Involvement of the nociceptin opioid peptide receptor in morphine-induced antinociception, tolerance and physical dependence in female mice.
Chen, JM; Hao, XQ; Li, J; Wang, ZY; Wu, N, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
rat metaboliteAny mammalian metabolite produced during a metabolic reaction in rat (Rattus norvegicus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
polypeptideA peptide containing ten or more amino acid residues.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nociceptin receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00060.00020.00060.0010AID389114; AID453416; AID453417; AID453418; AID453419
Mu-type opioid receptorHomo sapiens (human)Ki1.14740.00000.419710.0000AID150974; AID315427; AID367834; AID565968; AID621887
Delta-type opioid receptorHomo sapiens (human)Ki3.30770.00000.59789.9300AID148234; AID239157; AID315425; AID367836; AID565970; AID621888
Kappa-type opioid receptorHomo sapiens (human)Ki2.60780.00000.362410.0000AID148004; AID239074; AID315426; AID367835; AID565969; AID621889
Nociceptin receptorHomo sapiens (human)IC50 (µMol)0.00100.00010.12532.2000AID1167695; AID1167699; AID1167700; AID1285648; AID316812; AID340260; AID346443; AID453420; AID751863; AID752226
Nociceptin receptorHomo sapiens (human)Ki0.00020.00000.03370.5000AID1126451; AID1138770; AID147411; AID148869; AID148870; AID1820172; AID239061; AID239975; AID296542; AID315424; AID346443; AID367833; AID565967; AID621019; AID751863
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Translocator proteinRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00000.00350.0156AID368094
Delta-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.06310.00110.40144.8000AID148879
Kappa-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.06310.00080.80564.8860AID148879
Nociceptin receptorRattus norvegicus (Norway rat)EC50 (µMol)0.01600.00090.01470.0631AID148879; AID296546; AID389115; AID453408; AID453409; AID453411
Nociceptin receptorRattus norvegicus (Norway rat)Kd0.00040.00010.00040.0007AID148877; AID453421; AID453422; AID453423; AID453424
Nociceptin receptorMus musculus (house mouse)EC50 (µMol)0.00610.00090.00610.0115AID249516; AID296546; AID316813; AID541657
Kappa-type opioid receptorHomo sapiens (human)EC50 (µMol)0.07850.00000.22448.9900AID621023
Nociceptin receptorHomo sapiens (human)EC50 (µMol)0.00690.00010.00890.0630AID1138773; AID1302014; AID147763; AID148859; AID148860; AID148861; AID1810367; AID243147; AID246515; AID249517; AID296546; AID316813; AID368094; AID375525; AID453410; AID565965; AID621024
Nociceptin receptorHomo sapiens (human)Kd0.00010.00010.00010.0002AID1167694; AID453607
Mu-type opioid receptorMus musculus (house mouse)EC50 (µMol)0.06310.00020.03930.2030AID148879
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nociceptin receptorHomo sapiens (human)Kb0.00260.00030.00170.0050AID1126452
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
immune responseKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
chemical synaptic transmissionKappa-type opioid receptorHomo sapiens (human)
sensory perceptionKappa-type opioid receptorHomo sapiens (human)
locomotory behaviorKappa-type opioid receptorHomo sapiens (human)
sensory perception of painKappa-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
response to insulinKappa-type opioid receptorHomo sapiens (human)
positive regulation of dopamine secretionKappa-type opioid receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionKappa-type opioid receptorHomo sapiens (human)
response to nicotineKappa-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayKappa-type opioid receptorHomo sapiens (human)
maternal behaviorKappa-type opioid receptorHomo sapiens (human)
eating behaviorKappa-type opioid receptorHomo sapiens (human)
response to estrogenKappa-type opioid receptorHomo sapiens (human)
estrous cycleKappa-type opioid receptorHomo sapiens (human)
response to ethanolKappa-type opioid receptorHomo sapiens (human)
regulation of saliva secretionKappa-type opioid receptorHomo sapiens (human)
behavioral response to cocaineKappa-type opioid receptorHomo sapiens (human)
sensory perception of temperature stimulusKappa-type opioid receptorHomo sapiens (human)
defense response to virusKappa-type opioid receptorHomo sapiens (human)
cellular response to lipopolysaccharideKappa-type opioid receptorHomo sapiens (human)
cellular response to glucose stimulusKappa-type opioid receptorHomo sapiens (human)
positive regulation of p38MAPK cascadeKappa-type opioid receptorHomo sapiens (human)
positive regulation of potassium ion transmembrane transportKappa-type opioid receptorHomo sapiens (human)
response to acrylamideKappa-type opioid receptorHomo sapiens (human)
positive regulation of eating behaviorKappa-type opioid receptorHomo sapiens (human)
conditioned place preferenceKappa-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayKappa-type opioid receptorHomo sapiens (human)
calcium-mediated signalingNociceptin receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
sensory perceptionNociceptin receptorHomo sapiens (human)
sensory perception of painNociceptin receptorHomo sapiens (human)
response to estradiolNociceptin receptorHomo sapiens (human)
positive regulation of urine volumeNociceptin receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayNociceptin receptorHomo sapiens (human)
eating behaviorNociceptin receptorHomo sapiens (human)
negative regulation of cAMP-mediated signalingNociceptin receptorHomo sapiens (human)
estrous cycleNociceptin receptorHomo sapiens (human)
negative regulation of blood pressureNociceptin receptorHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayNociceptin receptorHomo sapiens (human)
regulation of locomotor rhythmNociceptin receptorHomo sapiens (human)
conditioned place preferenceNociceptin receptorHomo sapiens (human)
neuropeptide signaling pathwayNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor activityKappa-type opioid receptorHomo sapiens (human)
protein bindingKappa-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingKappa-type opioid receptorHomo sapiens (human)
dynorphin receptor activityKappa-type opioid receptorHomo sapiens (human)
neuropeptide bindingKappa-type opioid receptorHomo sapiens (human)
nociceptin receptor activityNociceptin receptorHomo sapiens (human)
G protein-coupled receptor activityNociceptin receptorHomo sapiens (human)
protein bindingNociceptin receptorHomo sapiens (human)
neuropeptide bindingNociceptin receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
plasma membraneKappa-type opioid receptorMus musculus (house mouse)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleoplasmKappa-type opioid receptorHomo sapiens (human)
mitochondrionKappa-type opioid receptorHomo sapiens (human)
cytosolKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
membraneKappa-type opioid receptorHomo sapiens (human)
sarcoplasmic reticulumKappa-type opioid receptorHomo sapiens (human)
T-tubuleKappa-type opioid receptorHomo sapiens (human)
dendriteKappa-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneKappa-type opioid receptorHomo sapiens (human)
presynaptic membraneKappa-type opioid receptorHomo sapiens (human)
perikaryonKappa-type opioid receptorHomo sapiens (human)
axon terminusKappa-type opioid receptorHomo sapiens (human)
postsynaptic membraneKappa-type opioid receptorHomo sapiens (human)
plasma membraneKappa-type opioid receptorHomo sapiens (human)
neuron projectionKappa-type opioid receptorHomo sapiens (human)
plasma membraneNociceptin receptorHomo sapiens (human)
cytoplasmic vesicleNociceptin receptorHomo sapiens (human)
plasma membraneNociceptin receptorHomo sapiens (human)
neuron projectionNociceptin receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (178)

Assay IDTitleYearJournalArticle
AID453424Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID148870Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
AID751863Binding affinity to human NOP receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID389118Stability in presence of rat brain trypsin assessed as half life of compound hydrolysis by HPLC2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID375525Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
AID389120Stability in presence of rat brain trypsin assessed as half life of compound hydrolysis in presence of trypsin inhibitor bacitracin by HPLC2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID148879pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor2000Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
AID389119Stability in presence of rat brain trypsin assessed compound degradation after 60 mins by HPLC2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID565968Displacement of [3H]DAMGO from human MOP receptor expressed in CHO-K1 cells after 45 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID565967Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID453608Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID1138770Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
AID367838Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID147414Stimulation of [35S]GTP-gamma-S, binding to human NOP receptor in cell membrane2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
AID453417Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID315425Displacement of [3H]naltrindole from human delta opioid receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID621020Selectivity ratio of Ki for human MOP receptor to Ki for human NOP receptor2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID1820169Displacement of [3H]-Diprenorphine from human MOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID641470Displacement of [3H]nociceptin from rat Galpha-fused ORL1 receptor expressed in african green monkey COS7 cells2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Capturing of the free cysteine residue in the ligand-binding site by affinity labeling of the ORL1 nociceptin receptor.
AID346443Displacement of radiolabeled nociceptin from human ORL1 receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
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.
AID541666Cytotoxicity in human erythrocytes assessed as induction of hemolysis at 100 uM2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice.
AID147406Concentration required to stimulate [35S]GTP-gamma-S, binding to human NOP receptor in cell membrane2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
AID1820167Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID367840Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID565966Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting relative to N/OFQ2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID565969Displacement of [3H]enadoline from human KOP receptor expressed in HEK-293 cells after 45 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID453610Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID296553Antagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID453422Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID367842Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding relative to DAMGO2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID453411Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID239975Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID249517Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID453413Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID541658Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay relative to control2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice.
AID1820168Displacement of [125I]-43RFa from human QRFP receptor expressed in CHO cells by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID389115Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID148234Binding affinity for opioid receptor type, human Opioid receptor delta 1 expressed in membrane homogenates of COS-1 or CHO cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID150974Binding affinity for opioid receptor type, human Opioid receptor mu 1 expressed in membrane homogenates of COS-1 or CHO cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID316812Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
AID316814Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to nociceptin2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
AID131274Tested for maximal effect induced by agonist1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide.
AID239895Antagonistic potency against N/OFQ induced GTPgammaS binding to human NOP receptor expressed in CHO cell membranes2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID453410Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID243147Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID453609Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID453415Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID148862Incorporation of [35S]GTP-gamma-S, into HEK293 membranes expressing human Opioid receptor like 12002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
AID367841Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to N/OFQ2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID453611Agonist activity at recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID240465Stimulation factor for GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP)2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID239074Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 12004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID148855% maximal activity against human Opioid receptor like 12002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID296551Antagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID1167697Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells at 10'-13 to 10'-5 M after 90 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID621887Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID566074Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in icv dosed Sprague-Dawley rat assessed as decrease of response threshold in contralateral paw after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID131279The maximal effect induced by an agonist expressed as percent inhibition of electrically induced twitches.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Structure-activity study of the nociceptin(1-13)-NH2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist.
AID239468Inhibition of [3H]diprenorphine binding to human Opioid receptor mu 1; ND denotes not determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID453409Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID453416Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID453419Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID453408Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID1820171Displacement of [3H]-Diprenorphine from human KOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1126451Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
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.
AID453412Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID316813Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
AID315424Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID752226Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
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.
AID296550Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID148860Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay2000Journal of medicinal chemistry, Apr-06, Volume: 43, Issue:7
High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
AID566071Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as assessed as minimum effective dose to increase of response threshold per site at 0.55 to 170 nmol/site, icv after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID1820166Displacement of [3H]-PrRP-20 from human PrRP receptor expressed in CHO cells by TopCount scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID1810369Agonist activity at human mu opioid receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
AID1167694Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID315428Selectivity for human NOP receptor over human kappa opioid receptor2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID453420Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID296549Antagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID245855Antagonistic potency against N/OFQ in electrically evoked contraction of mouse vas deferens2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID453607Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID247128Maximal inhibition of electrically evoked contraction of mouse vas deferens2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID1820172Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells by scintillation counting analysis2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID296552Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID453414Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay relative to wild type2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID367835Displacement of [3H]enadoline from human kappa opioid receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID246674Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor mu 1; ND denotes not determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID315426Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID566067Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as increase of response threshold per site at 0.55 to 170 nmol/site, icv after 1 hr2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID565980Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in intrathecally dosed Sprague-Dawley rat assessed as assessed as minimum effective dose to increase of response threshold per site after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID1820170Displacement of [3H]-Diprenorphine from human DOP receptor expressed in HEK293 cells by scintillation counting method2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Identification of an
AID315429Selectivity for human NOP receptor over human mu opioid receptor2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID375532Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization at up to 10 uM2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
AID247139Agonist activity as maximal effect in [35S]-GTP-gamma binding assay compared to 10 uM DAMGO; ND denotes not determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID621028Partial agonist activity at human NOP receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting relative to nociceptin2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID621026Partial agonist activity at human DOP receptor expressed in CHO cells assessed as maximal stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting relative to DPDPE2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID315427Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
AID389114Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID296542Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID296546Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID247133Maximum inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing human NOP receptor (CHOhNOP)2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID234615Effect of compound on nociceptin-induced allodynia :Values are the mean ( SE of allodynia score at 20 min.2000Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
AID148861Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 12002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID1126452Antagonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of nociceptin-induced [35S]-GTPgammaS binding after 2 hrs2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
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.
AID340260Inhibition of human ORL1 receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID565978Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in intrathecally dosed Sprague-Dawley rat assessed as increase of response threshold per site after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID1138768Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis relative to N/OFQ2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
AID367836Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHOK1 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID1167695Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID245854Antagonistic potency against N/OFQ in electrically evoked contractions of guinea pig ileum2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID139786Antagonist effect in the electrically stimulated mouse vas deferens; Not determined1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Structure-activity study of the nociceptin(1-13)-NH2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist.
AID566065Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as increase of response threshold per site at 0.55 to 55 nmol/site administered intrathecally after 1 hr2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID245853Antagonistic potency against forskolin stimulated cAMP levels in CHO cell membranes expressing human NOP receptor (CHOhNOP) at 1 uM2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID246515Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 12004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID148869Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID453423Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID565965Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID565964Agonist activity at human MOP receptor expressed in CHO-K1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID367844Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding relative to DPDPE2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID621889Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID565970Displacement of [3H]DPDPE from human DOP receptor expressed in CHO-K1 cells after 45 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID1810368Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay relative to control
AID239061Inhibition of [3H]nociceptin binding to human Opioid receptor like 12004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID1138773Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
AID566068Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as assessed as minimum effective dose to increase of response threshold per site at 0.55 to 170 nmol/site, icv after 1 hr2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID296548Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID621023Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID1167693Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells at 10 uM after 90 mins by scintillation counting analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID621024Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID1302014Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
AID566066Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as assessed as minimum effective dose to increase of response threshold per site at 0.55 to 55 nmol/site administered intrathecally after 2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID138538Tested for apparent affinity on electrically stimulated mouse vas deferens1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide.
AID566072Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as effect on allodynia in contralateral paw at 0.55 to 170 nmol/site administered intrathecally after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID453407Agonist activity at recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID453421Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID247135Agonist activity as maximal effect in [35S]-GTP-gamma binding assay compared to 60 nM N/OFQ2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID296547Antagonist activity at human NOP receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.
AID316817Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
AID389117Stability in presence of trypsin assessed as half life of compound hydrolysis2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation.
AID1285648Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID247125Maximal inhibition of electrically evoked contraction of guinea pig ileum2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID621019Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID453418Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation.
AID1167700Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID541657Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice.
AID566070Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as increase of response threshold per site at 0.55 to 170 nmol/site, icv after 20 mins2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID367834Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHOK1 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID1138783Displacement of [3H]Cl-DPDPE from human delta opioid receptor transfected in CHO cell membranes after 60 mins2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
AID367833Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID147763Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
AID249513Inhibition of electrically evoked contraction of guinea pig ileum2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID147411Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
The design and synthesis of a novel quinolizidine template for potent opioid and opioid receptor-like (ORL1, NOP) receptor ligands.
AID641473Displacement of [3H]nociceptin from rat Galpha-fused ORL1 receptor expressed in african green monkey COS7 cells preincubated with 100 uM N-ethylmaleimide for 90 mins measured after 90 mins2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Capturing of the free cysteine residue in the ligand-binding site by affinity labeling of the ORL1 nociceptin receptor.
AID566073Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in Sprague-Dawley rat assessed as effect on allodynia in contralateral paw at 0.55 to 170 nmol/site administered intrathecally after 1 hr2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID148004Binding affinity for opioid receptor type, human Opioid receptor kappa 1 expressed in membrane homogenates of COS-1 or CHO cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
AID1167698Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells at 10'-13 to 10'-5 M after 90 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID565962Agonist activity at human KOP receptor expressed in HEK-293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID621888Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
AID1167699Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID566075Antiallodynic activity against von Frey hair mechanically stimulated neuropathic pain in icv dosed Sprague-Dawley rat assessed as decrease of response threshold in contralateral paw after 1 hr2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
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: de
AID1810365Concentration ratio of human mu opioid receptor expressed in CHO cells to human NOP receptor expressed in CHO cells
AID368094Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID367843Agonist activity at human kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to enadoline2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID148859Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
AID316819Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction relative to control2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
AID139803Agonist effect in the electrically stimulated mouse vas deferens. (CL95%)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Structure-activity study of the nociceptin(1-13)-NH2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist.
AID1167701Ratio of IC50 for human ORL1 receptor high affinity binding site to IC50 for human ORL1 receptor high affinity binding site2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Tritium-labelled isovaleryl-RYYRIK-NH2 as potential antagonist probe for ORL1 nociceptin receptor.
AID148877Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 12000Bioorganic & medicinal chemistry letters, Apr-17, Volume: 10, Issue:8
ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
AID239157Inhibition of [3H]naltrindole binding to human Opioid receptor delta 12004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
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.
AID1810367Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
AID431278Ratio of EC50 for stimulation of [35S]GTPgammaS binding to rat ORL1 receptor expressed in african green monkey COS7 cells to IC50 for rat ORL1 receptor expressed in african green monkey COS7 cells2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Discriminatory synergistic effect of Trp-substitutions in superagonist [(Arg/Lys)(14), (Arg/Lys)(15)]nociceptin on ORL1 receptor binding and activation.
AID249516Inhibition of electrically evoked contraction of mouse vas deferens2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
AID367839Agonist activity at human kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
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 a
AID541665Half life in human serum2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice.
AID1346299Human NOP receptor (Opioid receptors)1997Neuropeptides, Oct, Volume: 31, Issue:5
Relationship between binding affinity and functional activity of nociceptin/orphanin FQ.
AID1346299Human NOP receptor (Opioid receptors)1997The Journal of pharmacology and experimental therapeutics, Nov, Volume: 283, Issue:2
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
AID1346299Human NOP receptor (Opioid receptors)1999British journal of pharmacology, May, Volume: 127, Issue:1
Comparison of the effects of [Phe1psi(CH2-NH)Gly2]nociceptin(1-13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors.
AID1346299Human NOP receptor (Opioid receptors)2002Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 365, Issue:6
Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues. 1. In vitro studies.
AID1346352Mouse NOP receptor (Opioid receptors)1997The Journal of pharmacology and experimental therapeutics, Nov, Volume: 283, Issue:2
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,274)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's293 (23.00)18.2507
2000's663 (52.04)29.6817
2010's270 (21.19)24.3611
2020's48 (3.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (0.46%)5.53%
Reviews122 (9.42%)6.00%
Case Studies1 (0.08%)4.05%
Observational1 (0.08%)0.25%
Other1,165 (89.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Pharmaco-Neuroimaging Studies of Approach/Avoidance Behaviors and Post-Mortem Studies: Study 1.1. (Pharmacological Manipulation) [NCT05232032]Phase 2112 participants (Anticipated)Interventional2023-07-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]