Therapeutic Targets Database
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TTD Target ID: TTDS00126

Target Information
NameMu-type opioid receptor    
Type of targetSuccessful target    
SynonymsMOR-1    
MOR1A    
Mu opioid receptor    
DiseaseAnalgesics    [1]
Cough    [2]
Diarrhea    [3]
Dyspnea    [4]
Opioid-induced bowel dysfunction    [5]
Pain, unspecified    [1]
Drug(s)AlfentanilApprovedAnesthetic[6]
AlvimopanApprovedPain[7]
AnileridineApprovedPain[8]
BuprenexApprovedPain[9]
BuprenorphineApprovedPain[9][10]
DiphenoxylateApprovedDiarrhea[11]
FentanylApprovedAnesthetic[12]
Levomethadyl AcetateApprovedOpiate dependence[13]
Methadyl AcetateApprovedOpiate dependence[14]
NaloxoneApprovedNarcotic depression[15][16]
OxymorphoneApprovedPain[17]
RemifentanilApprovedGeneral anesthesia[18]
MethylnaltrexonePhase IV completedConstipation, Postoperative ileus[19]
Tramadol ERPhase III completedNeuropathic pain, Postherpetic neuralgia[20]
GSK1521498Phase IObesity[21][22]
GNTIPreclinicalObesity[23]
LY-25582PreclinicalObesity[23]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP35372
FunctionInhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. The receptor for beta-endorphin.    
SequenceMDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Related US Patent6,451,806
6,680,071
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorC6S[24]
DC6S[24]
DM3A6S[24]
DM3B6S[24]
DM6S[24]
DPDPE[25]
Dimepheptanol[26]
Dynorphin (1-8)[27]
FALCARINDIOL[28]
FLUPERAMIDE[29]
GBR-12909[30]
ICI-199441[31]
ICI-199441[32]
KNT-5[33]
KNT-62[34]
KNT-63[34]
LY-255582[35]
M3A6S[24]
M3B6S[24]
M3IBu6S[24]
M3P6S[24]
M3Pr6S[24]
M3S[24]
M6S[24]
MC-CAM[36]
MCL-117[37]
MCL-139[37]
MCL-144[38]
MCL-145[37]
MCL-147[39]
MCL-149[39]
MCL-154[40]
MCL-182[39]
MCL-183[39]
MCL-428[41]
MCL-429[41]
MCL-431[41]
MCL-432[41]
MCL-433[41]
MCL-434[41]
MCL-435[41]
MCL-443[41]
MCL-444[41]
MCL-445[39]
MCL-446[39]
MCL-447[39]
MCL-448[39]
MCL-449[41]
MCL-450[42]
MCL-451[42]
MCL-457[39]
MCL-458[39]
MR-1029[43]
MR-1526[43]
MR-2034[44]
MR-2034[43]
MR-2266[43]
NalBzOH[24]
Naltrexone methiodide[45]
Naltrexone semicarbazone[27]
RTI-5989-31[46]
SB-0304[47]
SL-3111[48]
SN-11[49]
SN-23[49]
SN-28[50]
SNF-9007[51]
TRK-820[34]
U-69593[24]
UFP-502[52]
UFP-512[52]
beta-funaltrexamine[53]
AgonistAlfentanil[6]
Anileridine[8]
Buprenex[9]
Buprenorphine[9][10]
Carfentanil[54]
DBO-11[55]
DBO-17[55]
Dihydromorphine[56]
Dimethylthiambutene[57]
Diphenoxylate[11]
Ethylmorphine[58]
Etorphine[59]
Etorphine[60]
Fentanyl[12]
GSK1521498[21][22]
Levomethadyl Acetate[13]
Methadyl Acetate[14]
Oxymorphone[17]
Remifentanil[18]
Tramadol ER[20]
AntagonistAlvimopan[7]
Beta-endorphin[61]
Diprenorphine[62]
GNTI[23]
LY-25582[23]
Methylnaltrexone[19]
Naloxone[15][16]
MultitargetTramadol ER[20]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2Antitussive effect of nociceptin/orphanin FQ in experimental cough models. Pulm Pharmacol Ther. 2002;15(3):213-6. To Reference
Ref 3Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds. J Clin Gastroenterol. 2002 Jul;35(1 Suppl):S58-67. To Reference
Ref 4Lung opioid receptors: pharmacology and possible target for nebulized morphine in dyspnea. Life Sci. 2000;66(23):2221-31. To Reference
Ref 5Opioid-induced bowel dysfunction: pathophysiology and potential new therapies. Drugs. 2003;63(7):649-71. To Reference
Ref 6Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Pain. 2001 Mar;91(1-2):177-87. To Reference
Ref 7Alvimopan for postoperative ileus. Am J Health Syst Pharm. 2009 Jul 15;66(14):1267-77. To Reference
Ref 8Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 9Buprenorphine is a weak partial agonist that inhibits opioid receptor desensitization. J Neurosci. 2009 Jun 3;29(22):7341-8. To Reference
Ref 10Partial versus full agonists for opioid-mediated analgesia--focus on fentanyl and buprenorphine. Acta Anaesthesiol Belg. 2002;53(3):193-201. To Reference
Ref 11Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8. To Reference
Ref 12Opioid receptor mechanisms at the hypoglossal motor pool and effects on tongue muscle activity in vivo. J Physiol. 2009 Jun 1;587(Pt 11):2677-92. Epub 2009 Apr 29. To Reference
Ref 13Methadone-related opioid agonist pharmacotherapy for heroin addiction. History, recent molecular and neurochemical research and future in mainstream medicine. Ann N Y Acad Sci. 2000;909:186-216. To Reference
Ref 14Acetylmethadol metabolites influence opiate receptors and adenylate cyclase in amygdala. Eur J Pharmacol. 1981 Jul 10;72(4):343-9. To Reference
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Ref 17Simultaneous targeting of multiple opioid receptors: a strategy to improve side-effect profile. Br J Anaesth. 2009 Jul;103(1):38-49. Epub 2009 May 27. To Reference
Ref 18The pro-nociceptive effects of remifentanil or surgical injury in mice are associated with a decrease in delta-opioid receptor mRNA levels: Prevention of the nociceptive response by on-site delivery of enkephalins. Pain. 2009 Jan;141(1-2):88-96. Epub 2008 Dec 5. To Reference
Ref 19Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26. To Reference
Ref 20Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 21GSK. Product Development Pipeline. February 2009. To Reference
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Ref 24Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. To Reference
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Ref 32Bioorg 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
Ref 33Bioorg Med Chem Lett. 2010 Feb 1;20(3):1055-8. Epub 2009 Dec 26.Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology. To Reference
Ref 34Bioorg 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 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
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Ref 38J 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
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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 47J Med Chem. 2008 Apr 24;51(8):2571-4. Epub 2008 Mar 28.Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility. To Reference
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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
Ref 50Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. Epub 2010 Aug 21.Design and synthesis of KNT-127, a ¦Ä-opioid receptor agonist effective by systemic administration. To Reference
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Ref 52Bioorg Med Chem. 2010 Aug 15;18(16):6024-30. Epub 2010 Jun 25.Role of 2',6'-dimethyl-l-tyrosine (Dmt) in some opioid lead compounds. To Reference
Ref 53J Med Chem. 2009 Dec 10;52(23):7372-5.Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors. To Reference
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Ref 55Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71. To Reference
Ref 56Crooks PA, Kottayil SG, Al-Ghananeem AM, Byrn SR, Butterfield DA: Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13. To Reference
Ref 57Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 58Aasmundstad TA, Xu BQ, Johansson I, Ripel A, Bjorneboe A, Christophersen AS, Bodd E, Morland J: Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose. Br J Clin Pharmacol. 1995 Jun;39(6):611-20. To Reference
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Ref 60Internalization of mu-opioid receptors produced by etorphine in the rat locus coeruleus. Neuroscience. 2001;108(3):467-77. To Reference
Ref 61Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture. J Neurochem. 1993 Feb;60(2):765-7. To Reference
Ref 62Leung K: [6-O-methyl-11C]Diprenorphine To Reference



 

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