Therapeutic Targets Database
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TTD Target ID: TTDS00127

Target Information
NameKappa-type opioid receptor    
Type of targetSuccessful target    
SynonymsKOR    
KOR-1    
Kappa opioid receptor    
Opioid receptor Kappa    
DiseaseAlcohol dependence
[ICD9: 303   ICD10: F10.2]
[1]
Analgesics
[ICD9: 338   ICD10: R52]
[2]
Behcet's disease
[ICD9: 136.1   ICD10: M35.2]
[3]
Diarrhea
[ICD9: 787.91   ICD10: A09, K59.1]
[4]
Dyspnea
[ICD9: 786.09   ICD10: R06.0]
[5]
Focal ischemia
[ICD9: 459.89   ICD10: I99.8]
[6]
Immune disease[4]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[7]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[2]
Drug(s)DezocineApprovedPain[8]
AsimadolinePhase IIIDiarrhea Predominant Irritable Bowel Syndrome[9]
GNTIPreclinicalObesity[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP41145
PDB Structure2A0D; 2IQN; 4DJH.    
FunctionInhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. The receptor for dynorphins and may play a role in arousal and regulation of autonomic and neuroendocrine functions.    
SequenceMDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV RNTVQDPAYLRDIDGMNKPV
Related US Patent6,156,769
6,294,557
6,294,569
6,303,602
6,307,061
6,310,061
6,313,302
6,391,910
6,476,063
6,486,165
6,492,351
6,500,824
6,525,062
6,528,518
6,624,313
R,E38,,13
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-cyclorphan[11]
6-desoxonaltrexone[12]
6beta-naltrexol HCl[13]
ANISOCOUMARIN H[14]
BUTORPHAN[15]
BW-373U86,   SNC-86[16]
Benzyl derivative of M6G[17]
CCDC 710249, HCl salt[12]
CHLOROXINE[18]
CLIOQUINOL[18]
CYCLAZOCINE[15]
CYCLAZOCINE[19]
CYCLORPHAN[15]
DAMGO[20]
DM6S[20]
DPDPE[21]
DYNORPHIN A[22]
DYNORPHIN A[23]
Dimepheptanol[24]
Dynorphin (1-8)[25]
ELAEOCARPENINE[26]
ENDOMORPHIN 2[27]
ENDOMORPHIN-1[27]
ETONITAZENE[28]
FALCARINDIOL[14]
HERKINORIN[29]
ICI-199441[30]
ICI-199441[22]
ICI-204448[31]
KETOCYCLAZOCINE[32]
KNT-62[33]
KNT-63[33]
LOFENTANIL[34]
LY-255582[35]
M3A6S[20]
M3IBu6S[20]
M3P6S[20]
M3Pr6S[20]
M6S[20]
MC-CAM[36]
MCL-117[11]
MCL-139[11]
MCL-144[37]
MCL-145[11]
MCL-147[38]
MCL-149[38]
MCL-154[39]
MCL-182[38]
MCL-183[38]
MCL-428[40]
MCL-429[40]
MCL-431[40]
MCL-432[40]
MCL-433[40]
MCL-434[40]
MCL-435[40]
MCL-443[40]
MCL-444[40]
MCL-445[38]
MCL-446[38]
MCL-447[38]
MCL-448[38]
MCL-449[40]
MCL-450[41]
MCL-451[41]
MCL-457[38]
MCL-458[38]
METAZOCINE[32]
MK-1925[42]
MORPHINE SULFATE[24]
MR-1029[43]
MR-1526[43]
MR-2034[32]
MR-2034[43]
MR-2266[43]
NALFURAFINE[44]
NORBINALTORPHIMINE[44]
NalBzOH[20]
OXYMORPHINDOLE[45]
PHENAZOCINE[32]
RTI-5989-23[35]
RTI-5989-25[35]
RTI-5989-31[46]
SALVINICIN B[47]
SALVINORIN A[48]
SALVINORIN B[29]
SB-213698,   TAN-67[49]
SN-11[49]
SN-23[49]
SN-28[50]
Salvinorin A (ester)[51]
TRK-820[33]
U-69593[52]
ZYKLOPHIN[23]
[Leu5]enkephalin[53]
clocinnamox[54]
salvinicin A[47]
Agonist3-Methylfentanyl[55]
3-Methylthiofentanyl[56]
Asimadoline[9]
BRL 52537 hydrochloride[6]
BRL 52974[57]
Carfentanil[58]
Dihydromorphine[59]
Etorphine[60]
Fedotozine[4]
Nalorphine[61]
U-50488H[62]
U50,488H[1][62]
Antagonist7684380[63]
Beta-endorphin[64]
Dezocine[8]
Diprenorphine[65]
GNTI[10]
L-685,818[63]
Rapamycin[66]
[U-13C]ascomycin[67]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 4Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds. J Clin Gastroenterol. 2002 Jul;35(1 Suppl):S58-67. To Reference
Ref 5Lung opioid receptors: pharmacology and possible target for nebulized morphine in dyspnea. Life Sci. 2000;66(23):2221-31. To Reference
Ref 6Kappa-opioid receptor selectivity for ischemic neuroprotection with BRL 52537 in rats. Anesth Analg. 2003 Dec;97(6):1776-83. To Reference
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Ref 22Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71. Epub 2007 Dec 4.Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. To Reference
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Ref 24J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. To Reference
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Ref 26Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3. Epub 2010 Jan 22.Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs. To Reference
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Ref 28J Med Chem. 1990 Sep;33(9):2456-64.Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. To Reference
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Ref 30J Med Chem. 1996 Apr 12;39(8):1729-35.Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells. To Reference
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Ref 32Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. To Reference
Ref 33Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. Epub 2009 Nov 13.Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. To Reference
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Ref 35J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists. To Reference
Ref 36J Med Chem. 2009 Nov 12;52(21):6926-30.14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists. To Reference
Ref 37J Med Chem. 2009 Dec 10;52(23):7389-96.Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands. To Reference
Ref 38Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. To Reference
Ref 39Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors. To Reference
Ref 40Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors. To Reference
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Ref 42Bioorg Med Chem Lett. 2009 Aug 15;19(16):4729-32. Epub 2009 Jun 17.Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. To Reference
Ref 43J Med Chem. 1991 Aug;34(8):2438-44.Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers. To Reference
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Ref 45Eur J Med Chem. 2008 Nov;43(11):2307-15. Epub 2008 Feb 29.Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? To Reference
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Ref 47J Med Chem. 2007 Jul 26;50(15):3596-603. Epub 2007 Jun 20.Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues. To Reference
Ref 48J Med Chem. 2008 Mar 27;51(6):1824-30. Epub 2008 Feb 23.Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor. To Reference
Ref 49Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. To Reference
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Ref 54J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. To Reference
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Ref 61Apparent efficacy of kappa-opioid receptor ligands on serum prolactin levels in rhesus monkeys. Eur J Pharmacol. 1999 Nov 3;383(3):305-9. To Reference
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National University of Singapore, Singapore


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