Therapeutic Targets Database
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TTD Target ID: TTDS00128

Target Information
NameDelta-type opioid receptor    
Type of targetSuccessful target    
SynonymsDOR-1    
Delta opioid receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Cough
[ICD9: 786.2   ICD10: R05]
[2]
Dyspnea
[ICD9: 786.09   ICD10: R06.0]
[3]
Ischemia
[ICD9: 459.89   ICD10: I99.8]
[4]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[1]
Drug(s)ButorphanolApprovedPain[5]
CodeineApprovedPain[5]
HydrocodoneApprovedPain[2]
HydromorphoneApprovedPain[6]
LoperamideApprovedAcute nonspecific diarrhea[7]
NalbuphineApprovedPain[8]
NaltrexoneApprovedAlcohol dependence[9]
OxycodoneApprovedPain[10]
Divers drugPhase ICancer pain[11]
BIO-306PreclinicalAcute Ml[12]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP41143
PDB Structure1OZC; 2IQM.    
FunctionInhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective and receptor for enkephalins.    
SequenceMEPAPSAGAELQPPLFANASDAYPSAFPSAGANASGPPGARSASSLALAIAITALYSAVC AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC TPSDGPGGGAAA
Related US Patent6,630,462
6,680,318
6,790,854
Target ValidationClick to Find Target Validation Information.    
Inhibitor (-)-cyclorphan[13]
(-)-eseroline[14]
(-)-isoelaeocarpiline[15]
6-cinnamoylhernandine[16]
6-desoxonaltrexone[17]
6beta-naltrexol HCl[18]
8-carboxamidocyclazocine[19]
AKNADILACTAM[16]
AMINOFENTANYL[20]
BIPHALIN[21]
BUTORPHAN[22]
CARBOXYFENTANYL[23]
CYCLAZOCINE[24]
CYCLORPHAN[25]
DAMGO[26]
DELTORPHIN[27]
DELTORPHIN[28]
DELTORPHIN-II[29]
DERMORPHIN[30]
Dimepheptanol[31]
FALCARINDIOL[32]
GUANIDINONALTRINDOLE[33]
Grandisine C[15]
Grandisine F[15]
HERKINORIN[34]
ICI-174864[35]
ICI-174864[28]
ICI-199441[36]
ICI-199441[37]
MC-CAM[38]
MCL-117[13]
MCL-139[13]
MCL-144[39]
MCL-145[13]
MCL-147[40]
MCL-149[40]
MCL-153,   MCL-154[22]
MCL-154[22]
MCL-182[40]
MCL-183[40]
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[40]
MCL-446[40]
MCL-447[40]
MCL-448[40]
MCL-449[41]
MCL-450[42]
MCL-451[42]
MCL-458[40]
RTI-5989-23[43]
RTI-5989-25[43]
RTI-5989-31[44]
SALVINORIN A[34]
SB-0304[45]
SN-11[46]
SN-23[46]
SN-28[47]
SNF-9007[48]
UFP-502[29]
UFP-512[29]
[Leu5]enkephalin[49]
clocinnamox[50]
deltorphin C[30]
grandisine D[15]
Agonist3-Methylfentanyl[51]
3-Methylthiofentanyl[52]
BIO-306[12]
BW 373U86[53]
Beta-endorphin[54]
Butorphanol[5]
Carfentanil[55]
Codeine[5]
DADLE[4]
Dihydromorphine[56]
Dimethylthiambutene[57]
Divers drug[11]
Etorphine[58]
Etorphine[59]
Hydrocodone[2]
Oxycodone[10]
SB 227122[2]
SNC-80[60][1]
Tonazocine mesylate[1]
Antagonist7-benzylidenenaltrexone[61]
Diprenorphine[62]
HS 378[63]
ICI 154129[64]
Nalbuphine[8]
Naltrexone[9]
Naltrindole[61]
TIP[65]
TIPP[65]
BinderHydromorphone[6]
Loperamide[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2The antitussive activity of delta-opioid receptor stimulation in guinea pigs. J Pharmacol Exp Ther. 2000 Feb;292(2):803-9. To Reference
Ref 3Lung opioid receptors: pharmacology and possible target for nebulized morphine in dyspnea. Life Sci. 2000;66(23):2221-31. To Reference
Ref 4Delta opioid receptor stimulation mimics ischemic preconditioning in human heart muscle. J Am Coll Cardiol. 2000 Dec;36(7):2296-302. To Reference
Ref 5Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors. J Pharmacol Sci. 2005 Jun;98(2):109-16. Epub 2005 Jun 8. To Reference
Ref 6Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone]. J Med Chem. 2004 Mar 11;47(6):1400-12. To Reference
Ref 7Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8. To Reference
Ref 8Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. J Med Chem. 2007 May 3;50(9):2254-8. Epub 2007 Apr 4. To Reference
Ref 9Naltrexone reverses ethanol-induced dopamine release in the nucleus accumbens in awake, freely moving rats. Brain Res. 1993 Sep 3;621(1):137-40. To Reference
Ref 10Oxycodone: a pharmacological and clinical review. Clin Transl Oncol. 2007 May;9(5):298-307. To Reference
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Ref 12Pharmacologic therapeutics for cardiac reperfusion injury. Expert Opin Emerg Drugs. 2007 Sep;12(3):367-88. To Reference
Ref 13J 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
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Ref 15J Nat Prod. 2006 Sep;69(9):1295-9.Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis. To Reference
Ref 16J Nat Prod. 2010 May 28;73(5):988-91.Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica. To Reference
Ref 17Bioorg 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 18Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. Epub 2009 Mar 26.Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes. To Reference
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Ref 21Bioorg Med Chem. 2009 Oct 15;17(20):7337-43. Epub 2009 Aug 21.The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety. To Reference
Ref 22Bioorg 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 23J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors. To Reference
Ref 24Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. Epub 2008 Nov 24.Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. To Reference
Ref 25J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors. To Reference
Ref 26Bioorg. Med. Chem. 18(14):4975-4982 (2010) To Reference
Ref 27J Med Chem. 1994 Jan 7;37(1):146-50.Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors. To Reference
Ref 28J Med Chem. 1994 Jul 8;37(14):2125-8.Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist. To Reference
Ref 29Bioorg 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 30J Med Chem. 2005 Dec 29;48(26):8112-4.Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1). To Reference
Ref 31J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. To Reference
Ref 32Bioorg 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 33J Med Chem. 2003 Jul 3;46(14):3127-37.Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist. To Reference
Ref 34J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions. To Reference
Ref 35J Med Chem. 2006 Sep 7;49(18):5597-609.Highly potent and selective phenylmorphan-based inverse agonists of the opioid delta receptor. To Reference
Ref 36Bioorg Med Chem Lett. 2005 May 16;15(10):2647-52.Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity. To Reference
Ref 37Bioorg 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 38J 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 39J 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 40Bioorg 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 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. 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 44J 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 45J 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 46Bioorg 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 47Bioorg 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 48J 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 49J Med Chem. 2010 Apr 8;53(7):2875-81."Carba"-analogues of fentanyl are opioid receptor agonists. To Reference
Ref 50J 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
Ref 51Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM: Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. J Med Chem. 2000 Feb 10;43(3):381-91. To Reference
Ref 52You HJ, Colpaert FC, Arendt-Nielsen L: The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes. Exp Neurol. 2005 Jan;191(1):174-83. To Reference
Ref 53BW373U86, a delta opioid agonist, partially mediates delayed cardioprotection via a free radical mechanism that is independent of opioid receptor stimulation. J Mol Cell Cardiol. 2001 Aug;33(8):1455-65. To Reference
Ref 54Cross-linking of human [125I]beta-endorphin to opioid receptors in rat striatal membranes: biochemical evidence for the existence of a mu/delta opioid receptor complex. J Pharmacol Exp Ther. 1990 Apr;253(1):419-26. To Reference
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Ref 58Agonist-, antagonist-, and inverse agonist-regulated trafficking of the delta-opioid receptor correlates with, but does not require, G protein activation. J Pharmacol Exp Ther. 2001 Sep;298(3):1015-20. To Reference
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Ref 60Nonpeptidic delta-opioid receptor agonists reduce immobility in the forced swim assay in rats. Neuropsychopharmacology. 2002 Jun;26(6):744-55. To Reference
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Ref 62Leung K: [6-O-methyl-11C]Diprenorphine To Reference
Ref 63Binding, pharmacological and immunological profiles of the delta-selective opioid receptor antagonist HS 378. Life Sci. 2001 Aug 31;69(15):1775-82. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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