Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

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
Ref 1Clinical pharmacology of opioids for pain. Clin J Pain. 2002 Jul-Aug;18(4 Suppl):S3-13. To Reference
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
Ref 15OxyContin abuse and overdose. Postgrad Med. 2009 Mar;121(2):163-7. To Reference
Ref 16Mu opioid receptor antagonists: recent developments. ChemMedChem. 2007 Nov;2(11):1552-70. To Reference
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
Ref 222011 Pipeline of GlaxoSmithKline. To Reference
Ref 23Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
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
Ref 25Bioorg. Med. Chem. 18(14):4975-4982 (2010) To Reference
Ref 26J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. To Reference
Ref 27J Med Chem. 1986 Jul;29(7):1222-5.Peptides as receptor selectivity modulators of opiate pharmacophores. To Reference
Ref 28Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. To Reference
Ref 29Bioorg 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 30J Med Chem. 2001 Oct 11;44(21):3391-401.From hit to lead. Analyzing structure-profile relationships. To Reference
Ref 31J Med Chem. 1994 Sep 2;37(18):2856-64.Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide. To Reference
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
Ref 35Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. 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. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors. To Reference
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
Ref 39Bioorg 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 40Bioorg 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 41Bioorg 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
Ref 42J Med Chem. 2006 Sep 7;49(18):5640-3.New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores. 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
Ref 44Bioorg 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 45Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors. To Reference
Ref 46J Med Chem. 2007 Aug 9;50(16):3765-76. Epub 2007 Jul 11.Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series. To Reference
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
Ref 48J Med Chem. 1999 Dec 30;42(26):5359-68.Exploring the structure-activity relationships of [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective delta-opioid receptor nonpeptide agonist ligand. 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
Ref 50Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. Epub 2010 Aug 21.Design and synthesis of KNT-127, a -opioid receptor agonist effective by systemic administration. To Reference
Ref 51J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. To Reference
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
Ref 54Wax PM, Becker CE, Curry SC: Unexpected “gas” casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5. To Reference
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
Ref 59Duttaroy 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 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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

 
   
           
 
Computer-aided Drug Design
About BIDD | Databases | Software | Teaching | Research |  Links

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543