Therapeutic Targets Database
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TTD Target ID: TTDR01247

Target Information
NameNociceptin receptor    
Type of targetResearch target    
SynonymsKOR-3    
Kappa-type 3 opioid receptor    
OP(4)    
ORL-1    
ORL-1 receptor    
Opioid receptor 4    
Opioid receptor like-1 receptor    
Opioid-receptor-like 1    
Orphanin FQ receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1][2]
Anorexia nervosa
[ICD9: 307.1   ICD10: F50.0-F50.1]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Cerebral ischemia
[ICD9: 459.89   ICD10: I99.8]
[1]
Depression
[ICD9: 311   ICD10: F32]
[3]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
[1]
Epilepsy
[ICD9: 345   ICD10: G40]
[1]
Erectile dysfunction
[ICD9: 302.72, 607.84   ICD10: F52.2, N48.4]
[1]
Hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[1]
Neurogenic bladder
[ICD9: 188   ICD10: C67]
[1]
Neuropathic pain
[ICD9: 338,780   ICD10: R52, G89]
[1]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1][2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP41146
PDB Structure4EA3.    
FunctionReceptor for the neuropeptide nocipeptin/orphanin fq. Has a potential role in modulating a number of brain functions, including instinctive behaviors and emotions. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase.    
SequenceMEPLFPAPFWEVIYGSHLQGNLSLLSPNHSLLPPHLLLNASHGAFLPLGLKVTIVGLYLA VCVGGLLGNCLVMYVILRHTKMKTATNIYIFNLALADTLVLLTLPFQGTDILLGFWPFGN ALCKTVIAIDYYNMFTSTFTLTAMSVDRYVAICHPIRALDVRTSSKAQAVNVAIWALASV VGVPVAIMGSAQVEDEEIECLVEIPTPQDYWGPVFAICIFLFSFIVPVLVISVCYSLMIR RLRGVRLLSGSREKDRNLRRITRLVLVVVAVFVGCWTPVQVFVLAQGLGVQPSSETAVAI LRFCTALGYVNSCLNPILYAFLDENFKACFRKFCCASALRRDVQVSDRVRSIAKDVALAC KTSETVPRPA
Related US Patent6,340,681
6,410,561
6,423,725
Target ValidationClick to Find Target Validation Information.    
Inhibitor [Asp6,Lys10]N/OFQ (1-13)NH2[4]
cyclo [Asp6,Lys10]N/OFQ (1-13)NH2[4]
1- (1,2-diphenylethyl)-4-phenylpiperidin-4-ol[5]
1- (2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol[5]
1- (3,3-diphenylpropyl)-4-phenylpiperidin-4-ol[5]
1- (dio-tolylmethyl)-4-phenylpiperidin-4-ol[5]
1-benzhydryl-4- (2-fluorophenyl)piperidin-4-ol[6]
1-benzhydryl-4- (2-methoxyphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (3-fluorophenyl)piperidin-4-ol[6]
1-benzhydryl-4- (3-methoxyphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (3-phenylpropyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-bromophenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-butylphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-chlorophenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-ethylphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-fluorophenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-methoxyphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (4-propylphenyl)piperidin-4-ol[6]
1-benzhydryl-4- (benzyloxy)-4-phenylpiperidine[5]
1-benzhydryl-4- (furan-2-yl)piperidin-4-ol[6]
1-benzhydryl-4- (pyridin-2-yl)piperidin-4-ol[6]
1-benzhydryl-4- (thiophen-2-yl)piperidin-4-ol[6]
1-benzhydryl-4-benzylpiperidin-4-ol[6]
1-benzhydryl-4-butylpiperidin-4-ol[6]
1-benzhydryl-4-cyclohexylpiperidin-4-ol[6]
1-benzhydryl-4-cyclopropylpiperidin-4-ol[6]
1-benzhydryl-4-ethoxy-4-phenylpiperidine[5]
1-benzhydryl-4-hexylpiperidin-4-ol[6]
1-benzhydryl-4-isopropylpiperidin-4-ol[6]
1-benzhydryl-4-m-tolylpiperidin-4-ol[6]
1-benzhydryl-4-methoxy-4-phenylpiperidine[5]
1-benzhydryl-4-o-tolylpiperidin-4-ol[6]
1-benzhydryl-4-p-tolylpiperidin-4-ol[6]
1-benzhydryl-4-phenyl-4-propoxypiperidine[5]
1-benzhydryl-4-phenylpiperidin-4-ol[7]
1-benzhydryl-4-tert-butylpiperidin-4-ol[6]
1-benzyl-4-phenylpiperidin-4-ol[5]
2,2-diMeBut-RYYRIK-NH2[8]
2-MePen-RYYRIK-NH2[8]
3- (1-benzylpiperidin-4-yl)-5-chloro-1H-indole[9]
4- (2-[6]
4-phenyl-1- (1-phenylbutyl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylethyl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylheptyl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylhexyl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylpentyl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylpropan-2-yl)piperidin-4-ol[5]
4-phenyl-1- (1-phenylpropyl)piperidin-4-ol[5]
4-phenyl-1- (3-phenylpropyl)piperidin-4-ol[5]
4-phenyl-1- (phenyl[5]
4-phenyl-1- (phenyl[5]
4-phenyl-1- (phenyl[5]
4-phenyl-1- (phenyl[5]
4-phenyl-1- (phenyl[5]
Ac-Phe-[Orn-Pro-cha-Trp-Arg][10]
Ac-RYYRIK-GGG-K- (NH2)-YAFGYPS-GG[11]
Ac-RYYRIK-GGG-K- (NH2)-YRFB-GGGGG[11]
Ac-RYYRIK-K- (NH2)-YAFGYPS[11]
Ac-RYYRIK-K- (NH2)-YRFB[11]
Ac-RYYRIK-NH2[11]
Ac-RYYRIK-NH2[8]
Ada-RYYRIK-NH2[8]
Bu-RYYRIK-NH2[8]
Bz--RYYRIK-NH2[8]
CFGGFTCARKSARK[12]
CFGGFTCARKSARK[12]
CFGGFTGARKCARK[12]
CFGGFTGARKCARK[12]
EtBut-RYYRIK-NH2[8]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-Aib-N-Q-CONH2[13]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-Aib-N-Q-COOH[13]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-MeA-N-Q-CONH2[13]
F-G-G-F-T-G-A-R-K-S-A-R-K-L-MeA-N-Q-COOH[13]
F-G-G-F-T-G-A-R-K-S-Aib-R-K-L-A-N-Q-CONH2[13]
F-G-G-F-T-G-A-R-K-S-Aib-R-K-L-A-N-Q-COOH[13]
F-G-G-F-T-G-A-R-K-S-MeA-R-K-L-A-N-Q-CONH2[13]
F-G-G-F-T-G-A-R-K-S-MeA-R-K-L-A-N-Q-COOH[13]
F-G-G-F-T-G-Aib-R-K-S-A-R-K-L-A-N-Q-CONH2[13]
F-G-G-F-T-G-Aib-R-K-S-A-R-K-L-A-N-Q-COOH[13]
F-G-G-F-T-G-Aib-R-K-S-Aib-R-K-L-A-N-Q-CONH2[13]
F-G-G-F-T-G-MeA-R-K-S-A-R-K-L-A-N-Q-CONH2[13]
F-G-G-F-T-G-MeA-R-K-S-A-R-K-L-A-N-Q-COOH[13]
FGGFTCARKCARK[12]
FGGFTGARKCARKC[12]
FGGFTGARKCARKC[12]
FGGFTGARKRKRKLANQ[14]
FGGFTGARKSARK[12]
FGGFTGARKSARKAANQ[14]
FGGFTGARKSARKFANQ[14]
FGGFTGARKSARKKANQ[14]
FGGFTGARKSARKKKNQ[14]
FGGFTGARKSARKKRNQ[14]
FGGFTGARKSARKKWNQ[15]
FGGFTGARKSARKL[12]
FGGFTGARKSARKLADE[12]
FGGFTGARKSARKLARK[14]
FGGFTGARKSARKLFNQ[14]
FGGFTGARKSARKLKNQ[14]
FGGFTGARKSARKLLNQ[14]
FGGFTGARKSARKLRNQ[14]
FGGFTGARKSARKLVNQ[14]
FGGFTGARKSARKLWNQ[15]
FGGFTGARKSARKLYNQ[14]
FGGFTGARKSARKRANQ[14]
FGGFTGARKSARKRKNQ[15]
FGGFTGARKSARKRKRK[14]
FGGFTGARKSARKRRNQ[14]
FGGFTGARKSARKRWNQ[15]
FGGFTGARKSARKVANQ[14]
FGGFTGARKSARKWANQ[15]
FGGFTGARKSARKWKNQ[15]
FGGFTGARKSARKWRNQ[15]
FGGFTGARKSARKYANQ[14]
FGGFTGCRKSARKC[12]
FGGFTGCRKSARKC[12]
FGGFTGCRKSCRK[12]
FGGFTGCRKSCRK[12]
FGGFTRKRKSARKLANQ[14]
FLUPERAMIDE[16]
For-RYYRIK-NH2[8]
H-RYYRIK-NH2[8]
Hex-RYYRIK-NH2[8]
MeBut-RYYRIK-NH2[8]
NOCICEPTIN[14]
Piv-RYYRIK-NH2[8]
Pr-RYYRIK-NH2[8]
Va-RYYRIK-NH2[8]
[D-Asp7,Lys10]N/OFQ (1-13)NH2[4]
cyclo[Cys6,Cys10]N/OFQ (1-13)NH2[4]
cyclo[Cys7,Cys10]N/OFQ (1-13)NH2[4]
cyclo[DAsp7,Lys10]N/OFQ (1-13)NH2[4]
isoBu-RYYRIK-NH2[8]
isoVa-RYYRIK-NH2[8]
t-BuAc-RYYRIK-NH2[8]
AgonistEtorphine[17]
Ro-64-6198[1]
AntagonistJ-113397[18][1][3]
JTC-801[19]
JTC-801[20]
[Nphe (1)]-nociceptin [3]
AptamerNOX 2137a/b[21]
NOX 2149[21]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The nociceptin receptor as a potential target in drug design. Drug News Perspect. 2001 Aug;14(6):335-45. To Reference
Ref 2The opioid-receptor-like 1 (ORL-1) as a potential target for new analgesics. Eur J Med Chem. 2000 Mar;35(3):275-82. To Reference
Ref 3Nociceptin receptor antagonists display antidepressant-like properties in the mouse forced swimming test. Naunyn Schmiedebergs Arch Pharmacol. 2002 Feb;365(2):164-7. Epub 2001 Dec 20. To Reference
Ref 4J Med Chem. 2008 Aug 14;51(15):4385-7. Epub 2008 Jul 15.High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues. To Reference
Ref 5Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1. To Reference
Ref 6Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2. To Reference
Ref 7Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. Epub 2009 Mar 14.The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety. To Reference
Ref 8Bioorg Med Chem. 2008 Mar 1;16(5):2635-44. Epub 2007 Nov 21.Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist. To Reference
Ref 9Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. Epub 2006 Apr 24.3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor. To Reference
Ref 10Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. Epub 2006 Jul 28.Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. To Reference
Ref 11Bioorg Med Chem Lett. 2006 Sep 15;16(18):4839-41. Epub 2006 Jun 30.Synthesis and receptor binding properties of chimeric peptides containing a mu-opioid receptor ligand and nociceptin/orphanin FQ receptor ligand Ac-RYYRIK-amide. To Reference
Ref 12J Med Chem. 2001 Nov 8;44(23):4015-8.Structure-activity studies on nociceptin analogues: ORL1 receptor binding and biological activity of cyclic disulfide-containing analogues of nociceptin peptides. To Reference
Ref 13J Med Chem. 2002 Nov 21;45(24):5280-6.Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints. To Reference
Ref 14Bioorg Med Chem. 2008 Oct 15;16(20):9261-7. Epub 2008 Sep 9.Synergistic effect of basic residues at positions 14-15 of nociceptin on binding affinity and receptor activation. To Reference
Ref 15Bioorg Med Chem. 2009 Aug 1;17(15):5683-7. Epub 2009 Jun 13.Discriminatory synergistic effect of Trp-substitutions in superagonist [(Arg/Lys)(14), (Arg/Lys)(15)]nociceptin on ORL1 receptor binding and activation. To Reference
Ref 16Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9.Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. To Reference
Ref 17Duttaroy A, Yoburn BC: In vivo regulation of mu-opioid receptor density and gene expression in CXBK and outbred Swiss Webster mice. Synapse. 2000 Aug;37(2):118-24. To Reference
Ref 18Nocistatin and nociceptin given centrally induce opioid-mediated gastric mucosal protection. Peptides. 2008 Dec;29(12):2257-65. Epub 2008 Sep 26. To Reference
Ref 19Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71. To Reference
Ref 20Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009;23(2):301-3. Epub 2009 May 15. To Reference
Ref 21Therapeutic applications of aptamers. Expert Opin Investig Drugs. 2008 Jan;17(1):43-60. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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