Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00334

Target Information
NameCannabinoid receptor 1    
Type of targetSuccessful target    
SynonymsCANN6    
CB-R    
CB1    
Cannabinoid CB1 receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Inflammatory bowel disease
[ICD9: 555, 556   ICD10: K50, K51]
[2]
Migraine
[ICD9: 346   ICD10: G43]
[3]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Drug(s)MarinolApprovedAnorexia[4]
TebipenemPhase IINicotine dependence, Obesity[5]
TM38837Phase IObesity, metabolic disorders[6]
ZY01Phase IObesity, diabetes[7]
AVE1625Discontinued in Phase IISchizophrenia[8]
AZD1175Discontinued in Phase IHypertension; Diabetes/obesity[9]
AZD1704Terminated in Phase IPain[9]
AZD1940Discontinued in Phase IIAnalgaesia[9]
AZD2207Discontinued in Phase IDiabetes/obesity[9][10]
CBD cannabis derivativeDiscontinued in Phase ISchizophrenia[11]
CP-945598Discontinued in Phase IIIObesity[12]
Dianicline+rimonabantDiscontinuedTobacco dependence[13]
KDS-2000Discontinued in Phase IIPostherpetic neuralgia[14]
RimonabantWithdrawn by EMEA in 2009Obesity[15][16][17]
RimonbantWithdrawn in NDAObesity[18]
SLV-319Suspended in Phase IObesity, Psychosis[5]
TaranabantTerminated in Phase IIIObesity[15]
CB1 antagonistPreclinicalObesity[5]
JD-5037PreclinicalObesity, diabetes[19]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP21554
PDB Structure1LVQ; 1LVR; 2B0Y; 2KOE.    
FunctionInvolved in cannabinoid-induced cns effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide.    
SequenceMKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
Related US Patent6,509,367
6,525,087
6,642,258
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1R,2R)-N-Arachidonoylcyclopropanolamide[20]
(1R,2R)-N-Oleoylcyclopropanolamide[20]
(1R,2S)-N-Arachidonoylcyclopropanolamide[20]
2-Benzylbenzo[f]chromen-3-one[21]
3,4-diarylpyrazoline derivative[22]
4-cyanophenyl ethyl dodecylphosphonate[23]
A-796260[24]
AM-1241[24]
AM-1710[25]
AM-1714[25]
AM-1715[25]
AM-281[21]
AM-404[26]
AM-411[27]
AM-4768[25]
AM-630[28]
CP-4497,   CP-47497[29]
CP-55940[21]
DELTA 8-TETRAHYDROCANNOBINOL[30]
HU-210[31]
HU-210,   HU-211[32]
Isopropyl dodecylfluorophosphonate[33]
JWH-120[34]
JWH-133[35]
JWH-145[36]
JWH-146[36]
JWH-147[36]
JWH-150[36]
JWH-156[36]
JWH-229[34]
JWH-243[36]
JWH-244[36]
JWH-245[36]
JWH-246[36]
JWH-268[34]
JWH-292[36]
JWH-293[36]
JWH-297[37]
JWH-307[36]
JWH-308[36]
JWH-309[36]
JWH-324[29]
JWH-325[37]
JWH-337[37]
JWH-342[37]
JWH-342[29]
JWH-344[37]
JWH-345[37]
JWH-346[36]
JWH-347[36]
JWH-348[36]
JWH-363[36]
JWH-364[36]
JWH-365[36]
JWH-366[36]
JWH-367[36]
JWH-368[36]
JWH-369[36]
JWH-370[36]
JWH-371[36]
JWH-372[36]
JWH-373[36]
JWH-385[37]
JWH-392[37]
JWH-401[37]
JWH-402[37]
JWH-403[37]
JWH-404[37]
JWH-405[37]
JWH-406[37]
JWH-407[37]
JWH-440[29]
JWH-442[29]
KM-233[38]
KM-233[38]
KM-233[38]
KM-233-M[38]
MK-0364[39]
N- (4-methoxybenzyl)oleamide[40]
N- (4-methoxyphenethyl)oleamide[40]
N- (4-methoxyphenyl)oleamide[40]
N- (4-morpholinophenyl)docos-13-enamide[40]
N-octadecyl-N'-propylsulfamide[41]
NABILONE[42]
NAPHTHYRIDINONE[43]
OLEOYLETHANOLAMIDE[20]
PARAOXON[23]
PRAVADOLINE[44]
RIMONABANT HYDROCHLORIDE[31]
SCH-356036[45]
SEMIPLENAMIDE A[46]
SEMIPLENAMIDE B[46]
SR-144,528[47]
SR-147778[48]
Semiplenamide G[46]
TETRAHYDROLIPSTATIN[49]
VER-156084[50]
VER-156085[50]
VER-24052[50]
WIN-55212-2[21]
cis-N-oleoylcyclopropanolamide[20]
diethyl 3,5,6-trichloropyridin-2-yl phosphate[23]
dodecane-1-sulfonyl fluoride[23]
methyl icosylphosphonofluoridate[23]
octane-1-sulfonyl fluoride[23]
AgonistACEA[51]
AZD1940[9]
Anandamide[52]
Delta (9)-tetrahydrocannabinol[15]
Dianicline+rimonabant[13]
HU210[2]
JD-5037[19]
KDS-2000[14]
Marinol[4]
AntagonistAM-251[51]
AM251[3]
AVE1625[8]
AZD1175[9]
AZD1704[9]
AZD2207[9][10]
CB1 antagonist[5]
CBD cannabis derivative[11]
CP-945598[12]
Methanandamide[53]
Rimonabant[15][16][17]
Rimonbant[18]
SLV-319[5]
SR141716A[2][1]
TM38837[6]
Taranabant[15]
Tebipenem[5]
ZY01[7]
MultitargetSLV-319[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2The endogenous cannabinoid system protects against colonic inflammation. J Clin Invest. 2004 Apr;113(8):1202-9. To Reference
Ref 3Anandamide is able to inhibit trigeminal neurons using an in vivo model of trigeminovascular-mediated nociception. J Pharmacol Exp Ther. 2004 Apr;309(1):56-63. Epub 2004 Jan 12. To Reference
Ref 4Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol. 2009 Feb;156(3):397-411. To Reference
Ref 5Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
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Ref 11The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 12Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 13Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32. To Reference
Ref 14Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 15Central side-effects of therapies based on CB1 cannabinoid receptor agonists and antagonists: focus on anxiety and depression. Best Pract Res Clin Endocrinol Metab. 2009 Feb;23(1):133-44. To Reference
Ref 16End of the line for cannabinoid receptor 1 as an anti-obesity target? Nat Rev Drug Discov. 2008 Dec;7(12):961-2. To Reference
Ref 17Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
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Ref 21Bioorg Med Chem. 2009 Apr 1;17(7):2842-51. Epub 2009 Feb 21.Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. To Reference
Ref 22Bioorg Med Chem Lett. 2005 Nov 1;15(21):4794-8.Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. To Reference
Ref 23Bioorg Med Chem Lett. 2008 Nov 15;18(22):5875-8. Epub 2008 Aug 6.Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels. To Reference
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Ref 26J Med Chem. 1996 Oct 25;39(22):4515-9.Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand. To Reference
Ref 27J Med Chem. 2010 Aug 12;53(15):5656-66.Heteroadamantyl cannabinoids. To Reference
Ref 28Bioorg Med Chem Lett. 2007 Dec 1;17(23):6505-10. Epub 2007 Oct 1.New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. To Reference
Ref 29Bioorg Med Chem. 2010 Aug 1;18(15):5475-82. Epub 2010 Jun 22.Synthesis and pharmacology of 1-methoxy analogs of CP-47,497. To Reference
Ref 30J Med Chem. 2008 Oct 23;51(20):6393-9. Epub 2008 Oct 1.Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands. To Reference
Ref 31J Med Chem. 2006 Feb 9;49(3):872-82.Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists. To Reference
Ref 32J Med Chem. 2005 Nov 17;48(23):7486-90.1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists. To Reference
Ref 33Nat Chem Biol. 2008 Jun;4(6):373-8. Epub 2008 Apr 27.Activation of the endocannabinoid system by organophosphorus nerve agents. To Reference
Ref 34J Med Chem. 2009 Jan 22;52(2):369-78.Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow. To Reference
Ref 35Bioorg Med Chem. 2010 Nov 15;18(22):7809-15. Epub 2010 Sep 29.1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor. To Reference
Ref 36Bioorg Med Chem Lett. 2006 Oct 15;16(20):5432-5. Epub 2006 Aug 4.1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors. To Reference
Ref 37Bioorg Med Chem. 2008 Jan 1;16(1):322-35. Epub 2007 Sep 22.Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940. To Reference
Ref 38Bioorg Med Chem. 2008 Jul 1;16(13):6489-500. Epub 2008 May 20.Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs. To Reference
Ref 39J Med Chem. 2008 Apr 10;51(7):2108-14. Epub 2008 Mar 12.Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist. To Reference
Ref 40Bioorg Med Chem Lett. 2006 Jan 1;16(1):138-41. Epub 2005 Oct 6.New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies. To Reference
Ref 41Eur J Med Chem. 2009 Dec;44(12):4889-95. Epub 2009 Aug 12.Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide. To Reference
Ref 42J Med Chem. 2010 Oct 14;53(19):6996-7010.Novel 1',1'-chain substituted hexahydrocannabinols: 9-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist. To Reference
Ref 43Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. Epub 2010 Apr 21.Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation. To Reference
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Ref 45Bioorg Med Chem Lett. 2010 Feb 1;20(3):1084-9. Epub 2009 Dec 11.Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. To Reference
Ref 46J Nat Prod. 2003 Oct;66(10):1364-8.Semiplenamides A-G, fatty acid amides from a Papua New Guinea collection of the marine cyanobacterium Lyngbya semiplena. To Reference
Ref 47J Med Chem. 2006 Dec 14;49(25):7502-12.Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. To Reference
Ref 48J Med Chem. 2005 Aug 11;48(16):5059-87.The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. To Reference
Ref 49J Med Chem. 2008 Nov 13;51(21):6970-9. Epub 2008 Oct 3.Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism. To Reference
Ref 50Bioorg Med Chem Lett. 2009 Aug 1;19(15):4241-4. Epub 2009 May 29.Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. To Reference
Ref 51Posttraining activation of CB1 cannabinoid receptors in the CA1 region of the dorsal hippocampus impairs object recognition long-term memory. Neurobiol Learn Mem. 2008 Sep;90(2):374-81. Epub 2008 Jun 3. To Reference
Ref 52Opioid receptor and NO/cGMP pathway as a mechanism of peripheral antinociceptive action of the cannabinoid receptor agonist anandamide. Life Sci. 2009 Jul 1. [Epub ahead of print] To Reference
Ref 53Methanandamide attenuates cocaine-induced hyperthermia in rats by a cannabinoid CB(1)-dopamine D(2) receptor mechanism. Brain Res. 2009 Jan 17. [Epub ahead of print] To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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