Target Information

Target General Infomation
Target ID
T76685
Former ID
TTDS00334
Target Name
Cannabinoid receptor 1
Gene Name
CNR1
Synonyms
CANN6; CB-R; CB1; Cannabinoid CB1 receptor; CNR1
Target Type
Successful
Disease Anorexia [ICD9: 307.1; ICD10: F50.0-F50.1]
Central nervous system disease [ICD10: G00-G99]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Chemotherapy-induced nausea [ICD9: 787, 787.0; ICD10: R11]
Diabetes; Obesity [ICD9: 250, 278; ICD10: E08-E13, E66]
Drug abuse [ICD9: 303-304; ICD10: F10-F19]
Endocrine disease [ICD10: E00-E35]
Hypertension; Diabetes; Obesity [ICD9: 250, 278, 401; ICD10: E08-E13, E66, I10-I16]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Ischemia [ICD9: 459.89; ICD10: I99.8]
Lipid metabolism disorder [ICD10: E75-E78]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Nicotine dependence; Obesity [ICD9: 278, 305.1; ICD10: E66, F17]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Ovarian cancer [ICD9: 183; ICD10: C56]
Obesity [ICD9: 278; ICD10: E66]
Obesity; Metabolic disorders [ICD9: 270-279, 278; ICD10: E66, E70-E89]
Obesity; Diabetes [ICD9: 250, 278; ICD10: E08-E13, E66]
Postherpetic neuralgia [ICD9: 53.19; ICD10: B02.2, G44.847, G53.0]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Schizophrenia [ICD9: 295; ICD10: F20]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Tobacco dependence [ICD9: 305.1; ICD10: F17]
Function
Involved in cannabinoid-induced cns effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide.
BioChemical Class
GPCR rhodopsin
Target Validation
T76685
UniProt ID
P21554
Sequence
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
Drugs and Mode of Action
Drug(s) Marinol Drug Info Approved Anorexia [538510]
NABILONE Drug Info Approved Insomnia [551871]
SR141716A Drug Info Approved Obesity [546366], [551871]
TETRAHYDROLIPSTATIN Drug Info Approved Obesity [545361], [551871]
Dronabinol oral solution Drug Info Phase 2/3 Chemotherapy-induced nausea [551036]
GW-42004 Drug Info Phase 2 Lipid metabolism disorder [549419]
SR-147778 Drug Info Phase 2 Obesity [521745]
Tebipenem Drug Info Phase 2 Nicotine dependence; Obesity [536122]
TM38837 Drug Info Phase 1 Obesity; Metabolic disorders [543260], [550186]
V-24343 Drug Info Phase 1 Type 2 diabetes [522402]
ZY01 Drug Info Phase 1 Obesity; Diabetes [551790]
CB1 antagonist, Bayer Drug Info Preclinical Obesity [536122]
JD-5037 Drug Info Preclinical Obesity; Diabetes [551059]
Rimonabant Drug Info Withdrawn from market Obesity [537145], [542474]
Rimonbant Drug Info Withdrawn from market Obesity [536710]
CP-945598 Drug Info Discontinued in Phase 3 Obesity [536122]
Taranabant Drug Info Discontinued in Phase 3 Obesity [537068]
AVE1625 Drug Info Discontinued in Phase 2 Psychotic disorders [547945]
AZD1940 Drug Info Discontinued in Phase 2 Pain [548585]
AZD2207 Drug Info Discontinued in Phase 2 Diabetes; Obesity [548462]
KDS-2000 Drug Info Discontinued in Phase 2 Postherpetic neuralgia [536374]
KN-38-7271 Drug Info Discontinued in Phase 2 Ischemia [547265]
SLV319 Drug Info Discontinued in Phase 2 Obesity [547594]
AZD1175 Drug Info Discontinued in Phase 1 Hypertension; Diabetes; Obesity [548277]
AZD1704 Drug Info Discontinued in Phase 1 Pain [548792]
CBD cannabis derivative Drug Info Discontinued in Phase 1 Schizophrenia [536463]
PF-514273 Drug Info Discontinued in Phase 1 Obesity [548445]
TAK-937 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [548963]
Dianicline+rimonabant Drug Info Terminated Tobacco dependence [548622]
WIN-55212-2 Drug Info Terminated Discovery agent [542353], [545702]
Inhibitor (1R,2R)-N-Arachidonoylcyclopropanolamide Drug Info [530070]
(1R,2R)-N-Oleoylcyclopropanolamide Drug Info [530070]
(1R,2S)-N-Arachidonoylcyclopropanolamide Drug Info [530070]
(1R,2S)-N-Oleoylcyclopropanolamide Drug Info [530070]
(1S,2R)-N-Oleoylcyclopropanolamide Drug Info [530070]
(1S,2S)-N-Arachidonoylcyclopropanolamide Drug Info [530070]
(1S,2S)-N-Oleoylcyclopropanolamide Drug Info [530070]
(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
(4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone Drug Info [530617]
(E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide Drug Info [527788]
(E)-N-(4-methoxyphenethyl)undec-2-enamide Drug Info [527788]
(E)-N-(4-methoxyphenyl)undec-2-enamide Drug Info [527788]
1,3,5-triphenylimidazolidine-2,4-dione Drug Info [527995]
1,3,5-tris(4-chlorophenyl)imidazolidine-2,4-dione Drug Info [527995]
1,4-dihydroindeno[1,2-c]-pyrazole Drug Info [527858]
1,5-bis(4-chlorophenyl)-1H-1,2,3-triazole Drug Info [529882]
1-(2-morpholinoethyl)-1H-indol-3-yl acetate Drug Info [528907]
1-(4-CHLOROPHENYL)-2-(2,4-DICHLOROPHENYL)-5-(METHYLSULFINYL)-N-(PIPERIDIN-1-YL)-1H-IMIDAZOLE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info [530827]
1-(bis(4-bromophenyl)methyl)-3-phenylurea Drug Info [527861]
1-(bis(4-chlorophenyl)methyl)-3-phenylurea Drug Info [527861]
1-[bis(4-bromophenyl)methyl]-3-phenylthiourea Drug Info [527861]
1-[bis(4-chlorophenyl)methyl]-3-(4-chlorophenyl)- Drug Info [527861]
1-[bis(4-chlorophenyl)methyl]-3-phenylthiourea Drug Info [527861]
1-[bis(4-iodophenyl)methyl]-3-(4-bromophenyl)urea Drug Info [527861]
2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info [528844]
2-Benzylbenzo[f]chromen-3-one Drug Info [530009]
3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info [528844]
3,4-diarylpyrazoline derivative Drug Info [527721]
3-Benzyl-5-isopropyl-8-methylchromen-2-one Drug Info [530009]
3-Benzyl-5-methoxy-7-methylchromen-2-one Drug Info [530009]
3-Benzyl-5-methoxychromen-2-one Drug Info [530009]
4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info [528844]
4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol Drug Info [528844]
4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol Drug Info [528844]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-benzhydryl-N-butylpiperazine-1-carboxamide Drug Info [530617]
4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide Drug Info [530617]
4-cyanophenyl ethyl dodecylphosphonate Drug Info [529659]
5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol Drug Info [528844]
5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole Drug Info [529434]
5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one Drug Info [530009]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
A-796260 Drug Info [530525]
AM-1241 Drug Info [530525]
AM-1710 Drug Info [529170]
AM-1714 Drug Info [529170]
AM-1715 Drug Info [529170]
AM-281 Drug Info [530009]
AM-404 Drug Info [534262]
AM-411 Drug Info [531004]
AM-4768 Drug Info [529170]
AM-630 Drug Info [529106]
Chlorphrifos oxon Drug Info [529659]
Cis-N-oleoylcyclopropanolamide Drug Info [530070]
CP-4497 Drug Info [531027]
CP-55940 Drug Info [530009]
DELTA 8-TETRAHYDROCANNOBINOL Drug Info [529727]
Dodecane-1-sulfonyl fluoride Drug Info [529659]
Isopropyl 4-nitrophenyl dodecylphosphonate Drug Info [529659]
Isopropyl dodecylfluorophosphonate Drug Info [529440]
JWH-120 Drug Info [529920]
JWH-133 Drug Info [531214]
JWH-145 Drug Info [528355]
JWH-146 Drug Info [528355]
JWH-147 Drug Info [528355]
JWH-150 Drug Info [528355]
JWH-156 Drug Info [528355]
JWH-229 Drug Info [529920]
JWH-243 Drug Info [528355]
JWH-244 Drug Info [528355]
JWH-245 Drug Info [528355]
JWH-246 Drug Info [528355]
JWH-268 Drug Info [529920]
JWH-292 Drug Info [528355]
JWH-293 Drug Info [528355]
JWH-297 Drug Info [529084]
JWH-307 Drug Info [528355]
JWH-308 Drug Info [528355]
JWH-309 Drug Info [528355]
JWH-324 Drug Info [531027]
JWH-325 Drug Info [529084]
JWH-337 Drug Info [529084]
JWH-342 Drug Info [529084]
JWH-344 Drug Info [529084]
JWH-345 Drug Info [529084]
JWH-346 Drug Info [528355]
JWH-347 Drug Info [528355]
JWH-348 Drug Info [528355]
JWH-363 Drug Info [528355]
JWH-364 Drug Info [528355]
JWH-365 Drug Info [528355]
JWH-366 Drug Info [528355]
JWH-367 Drug Info [528355]
JWH-368 Drug Info [528355]
JWH-369 Drug Info [528355]
JWH-370 Drug Info [528355]
JWH-371 Drug Info [528355]
JWH-372 Drug Info [528355]
JWH-373 Drug Info [528355]
JWH-385 Drug Info [529084]
JWH-392 Drug Info [529084]
JWH-401 Drug Info [529084]
JWH-402 Drug Info [529084]
JWH-403 Drug Info [529084]
JWH-404 Drug Info [529084]
JWH-405 Drug Info [529084]
JWH-406 Drug Info [529084]
JWH-407 Drug Info [529084]
JWH-440 Drug Info [531027]
JWH-442 Drug Info [531027]
KM-233 Drug Info [529515]
KM-233-M Drug Info [529515]
Methyl icosylphosphonofluoridate Drug Info [529659]
N-(1-adamantyl)-N'-propylsulfamide Drug Info [530389]
N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide Drug Info [529838]
N-(2,4-dimethoxyphenethyl)docos-13-enamide Drug Info [527788]
N-(2,4-dimethoxyphenethyl)oleamide Drug Info [527788]
N-(2-adamantyl)-N'-propylsulfamide Drug Info [530389]
N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide Drug Info [529106]
N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide Drug Info [529563]
N-(3,3-Diphenyl)propyl-2-phenylacetamide Drug Info [529563]
N-(3,5-dimethoxyphenethyl)docos-13-enamide Drug Info [527788]
N-(3,5-dimethoxyphenethyl)oleamide Drug Info [527788]
N-(3-Phenyl)propyl-2,2-diphenylacetamide Drug Info [529563]
N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) Drug Info [529563]
N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide Drug Info [529838]
N-(4-methoxybenzyl)oleamide Drug Info [527788]
N-(4-methoxyphenethyl)oleamide Drug Info [527788]
N-(4-methoxyphenyl)oleamide Drug Info [527788]
N-(4-morpholinophenyl)docos-13-enamide Drug Info [527788]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Drug Info [530929]
N-(cis-9-cis-12-octadecadienyl)sulfamide Drug Info [530389]
N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info [528112]
N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine Drug Info [528112]
N-ethyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info [528851]
N-isopentyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info [528851]
N-isopropyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info [528851]
N-methyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info [528851]
N-octadecyl-N'-propylsulfamide Drug Info [530389]
N-phenyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info [528851]
N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) Drug Info [530871]
NABILONE Drug Info [531196]
NAPHTHYRIDINONE Drug Info [530929]
O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info [528112]
Octane-1-sulfonyl fluoride Drug Info [529659]
OLEOYLETHANOLAMIDE Drug Info [530070]
PARAOXON Drug Info [529659]
PRAVADOLINE Drug Info [551296]
Rac-cis-N-arachidonoylcyclopropanolamide Drug Info [530070]
Rac-trans-N-oleoylcyclopropanolamide Drug Info [530070]
SCH-356036 Drug Info [530597]
SEMIPLENAMIDE A Drug Info [526859]
SEMIPLENAMIDE B Drug Info [526859]
Semiplenamide G Drug Info [526859]
TETRAHYDROLIPSTATIN Drug Info [529733]
VER-156084 Drug Info [530200]
VER-156085 Drug Info [530200]
WIN-55212-2 Drug Info [530009]
{[(9Z)-octadec-9-en-1-yl]sulfamoyl}amine Drug Info [530389]
Agonist ACEA Drug Info [536731]
Anandamide Drug Info [537577]
arachidonyl-2-chloroethylamide Drug Info [525498]
arachidonylcyclopropylamide Drug Info [525498]
AZ-599 Drug Info [543877]
AZD1940 Drug Info [550288]
cannabinol Drug Info [534216]
Delta(9)-tetrahydrocannabinol Drug Info [537149]
Dianicline+rimonabant Drug Info [537145]
Dibenzothiazepines Drug Info [543877]
HU210 Drug Info [535946]
JD-5037 Drug Info [551059]
KDS-2000 Drug Info [536374]
Marinol Drug Info [537087]
MK-5596 Drug Info [543877]
O-1812 Drug Info [525966]
[3H]CP55940 Drug Info [534130]
[3H]HU-243 Drug Info [526736]
[3H]WIN55212-2 Drug Info [534535]
Antagonist AM251 Drug Info [535887]
AVE1625 Drug Info [549823]
AZD1175 Drug Info [550288]
AZD1704 Drug Info [550288]
AZD2207 Drug Info [550288], [551589]
BMS-812204 Drug Info [543877]
Cannabinoid 1 antagonists Drug Info [543877]
CB1 antagonist, Bayer Drug Info [536122]
CB1 antagonists Drug Info [543877]
CB1 antagonists Drug Info [543877]
CBD cannabis derivative Drug Info [536463]
compound 70 Drug Info [533285]
CP-945598 Drug Info [549974]
CXB-029 Drug Info [543877]
LY320135 Drug Info [534541]
Methanandamide Drug Info [537268]
Rimonabant Drug Info [536549], [536956], [537149]
Rimonbant Drug Info [536710]
SLV319 Drug Info [532030]
SR141716A Drug Info [535198], [535946]
Taranabant Drug Info [537149]
Tebipenem Drug Info [536122]
TM38837 Drug Info [550186]
V-24343 Drug Info [529987]
ZY01 Drug Info [551790]
[123I]AM251 Drug Info [534489]
Modulator Dronabinol oral solution Drug Info [1572591]
GW-42004 Drug Info
KN-38-7271 Drug Info
PF-514273 Drug Info [532853]
SR-147778 Drug Info
TAK-937 Drug Info [531715]
Modulator (allosteric modulator) Org27569 Drug Info [531899]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Rap1 signaling pathway
Neuroactive ligand-receptor interaction
Retrograde endocannabinoid signaling
PANTHER Pathway Endogenous cannabinoid signaling
Pathway Interaction Database N-cadherin signaling events
Reactome Class A/1 (Rhodopsin-like receptors)
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Small Ligand GPCRs
BDNF signaling pathway
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 521745ClinicalTrials.gov (NCT00239174) A Multicenter Study to Evaluate the Efficacy and Safety of of Four Doses of SR147778 in Obese Patients. U.S. National Institutes of Health.
Ref 522402ClinicalTrials.gov (NCT00734201) Safety and Efficacy of Low Doses of V24343 in Obese Subjects. U.S. National Institutes of Health.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 537068Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
Ref 537145Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32.
Ref 538510FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018651.
Ref 542353(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 733).
Ref 542474(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 745).
Ref 543260(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8705).
Ref 545361Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003007)
Ref 545702Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004262)
Ref 546366Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007737)
Ref 547265Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014615)
Ref 547594Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017654)
Ref 547945Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020616)
Ref 548277Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024090)
Ref 548445Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025584)
Ref 548462Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025707)
Ref 548585Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026807)
Ref 548622Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143)
Ref 548792Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028889)
Ref 548963Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030875)
Ref 549419Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036909)
Ref 5501862011 Pipeline of 7TM Pharma.
Ref 551036Clinical pipeline report, company report or official report of INSYS Therapeutics.
Ref 5510592011 Pipeline of Jenrin Discovery.
Ref 5517902011 Pipeline of Zydus Cadila Group.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525498Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1). J Pharmacol Exp Ther. 1999 Jun;289(3):1427-33.
Ref 525966Highly selective CB(1) cannabinoid receptor ligands and novel CB(1)/VR(1) vanilloid receptor "hybrid" ligands. Biochem Biophys Res Commun. 2001 Feb 23;281(2):444-51.
Ref 526736A novel probe for the cannabinoid receptor. J Med Chem. 1992 May 29;35(11):2065-9.
Ref 526859J 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.
Ref 527721Bioorg Med Chem Lett. 2005 Nov 1;15(21):4794-8.Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity.
Ref 527788Bioorg 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.
Ref 527858J Med Chem. 2005 Nov 17;48(23):7351-62.Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide.
Ref 527861J 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.
Ref 527995J 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 receptorinverse agonists/antagonists.
Ref 528112J Med Chem. 2006 Apr 6;49(7):2333-8.Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.
Ref 528355Bioorg 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.
Ref 528844Bioorg Med Chem Lett. 2007 Jul 1;17(13):3652-6. Epub 2007 Apr 25.Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.
Ref 528851Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. Epub 2007 Apr 29.Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Ref 528907Eur J Med Chem. 2008 Mar;43(3):513-39. Epub 2007 May 6.Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.
Ref 529084Bioorg 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.
Ref 529106Bioorg 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.
Ref 529170J Med Chem. 2007 Dec 27;50(26):6493-500. Epub 2007 Nov 27.Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.
Ref 529434Bioorg Med Chem Lett. 2008 May 1;18(9):2820-4. Epub 2008 Apr 4.New tetrazole-based selective anandamide uptake inhibitors.
Ref 529440Nat Chem Biol. 2008 Jun;4(6):373-8. Epub 2008 Apr 27.Activation of the endocannabinoid system by organophosphorus nerve agents.
Ref 529515Bioorg 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.
Ref 529563Bioorg Med Chem. 2008 Aug 1;16(15):7510-5. Epub 2008 Jun 7.Novel sterically hindered cannabinoid CB1 receptor ligands.
Ref 529659Bioorg Med Chem Lett. 2008 Nov 15;18(22):5875-8. Epub 2008 Aug 6.Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
Ref 529727J Med Chem. 2008 Oct 23;51(20):6393-9. Epub 2008 Oct 1.Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands.
Ref 529733J Med Chem. 2008 Nov 13;51(21):6970-9. Epub 2008 Oct 3.Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism.
Ref 529838J Med Chem. 2008 Dec 25;51(24):7800-5.New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.
Ref 529882Bioorg Med Chem Lett. 2009 Feb 1;19(3):891-3. Epub 2008 Dec 6.Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles.
Ref 529920J Med Chem. 2009 Jan 22;52(2):369-78.Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.
Ref 529987Cannabinoid receptor antagonists: pharmacological opportunities, clinical experience, and translational prognosis. Expert Opin Emerg Drugs. 2009 Mar;14(1):43-65.
Ref 530009Bioorg 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.
Ref 530070J Med Chem. 2009 May 14;52(9):3001-9.Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Ref 530200Bioorg 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.
Ref 530389Eur J Med Chem. 2009 Dec;44(12):4889-95. Epub 2009 Aug 12.Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide.
Ref 530525J Med Chem. 2010 Jan 14;53(1):295-315.Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Ref 530597Bioorg 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.
Ref 530617Eur J Med Chem. 2010 Mar;45(3):1133-9. Epub 2009 Dec 16.Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
Ref 530827Bioorg Med Chem Lett. 2010 May 1;20(9):2770-5. Epub 2010 Mar 19.Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern.
Ref 530871J Med Chem. 2010 May 27;53(10):4028-37.Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Ref 530929Bioorg 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.
Ref 531004J Med Chem. 2010 Aug 12;53(15):5656-66.Heteroadamantyl cannabinoids.
Ref 531027Bioorg Med Chem. 2010 Aug 1;18(15):5475-82. Epub 2010 Jun 22.Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531196J Med Chem. 2010 Oct 14;53(19):6996-7010.Novel 1',1'-chain substituted hexahydrocannabinols: 9|A-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist.
Ref 531214Bioorg 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.
Ref 531715Cerebroprotective effects of TAK-937, a cannabinoid receptor agonist, on ischemic brain damage in middle cerebral artery occluded rats and non-human primates. Brain Res. 2012 Jan 9;1430:93-100.
Ref 531899Indole-2-carboxamides as allosteric modulators of the cannabinoid CB??receptor. J Med Chem. 2012 Jun 14;55(11):5627-31.
Ref 532030JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6173-80.
Ref 532853Effects of the novel cannabinoid CB1 receptor antagonist PF 514273 on the acquisition and expression of ethanol conditioned place preference. Alcohol. 2014 Aug;48(5):427-31.
Ref 533285A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents. Expert Opin Ther Pat. 2015 Oct;25(10):1093-116.
Ref 534130Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A. J Biol Chem. 1996 Mar 22;271(12):6941-6.
Ref 534216Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands. J Pharmacol Exp Ther. 1996 Sep;278(3):989-99.
Ref 534262J Med Chem. 1996 Oct 25;39(22):4515-9.Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand.
Ref 534489Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci. 1997;61(14):PL 191-7.
Ref 534535Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1. J Neurochem. 1998 Jan;70(1):366-73.
Ref 534541LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan;284(1):291-7.
Ref 535198Antinociceptive activity of the endogenous fatty acid amide, palmitylethanolamide. Eur J Pharmacol. 2001 May 11;419(2-3):191-8.
Ref 535887Anandamide 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.
Ref 535946The endogenous cannabinoid system protects against colonic inflammation. J Clin Invest. 2004 Apr;113(8):1202-9.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536549Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 536731Posttraining 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.
Ref 536956End of the line for cannabinoid receptor 1 as an anti-obesity target? Nat Rev Drug Discov. 2008 Dec;7(12):961-2.
Ref 537087Emerging strategies for exploiting cannabinoid receptor agonists as medicines. Br J Pharmacol. 2009 Feb;156(3):397-411.
Ref 537145Emerging drugs for the treatment of tobacco dependence. Expert Opin Emerg Drugs. 2009 Mar;14(1):23-32.
Ref 537149Central 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.
Ref 537268Methanandamide attenuates cocaine-induced hyperthermia in rats by a cannabinoid CB(1)-dopamine D(2) receptor mechanism. Brain Res. 2009 Jan 17.
Ref 537577Opioid receptor and NO/cGMP pathway as a mechanism of peripheral antinociceptive action of the cannabinoid receptor agonist anandamide. Life Sci. 2009 Jul 1.
Ref 543877(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 56).
Ref 549823Pharma & Vaccines. Product Development Pipeline. April 29 2009.
Ref 549974Pfizer. Product Development Pipeline. March 31 2009.
Ref 5501862011 Pipeline of 7TM Pharma.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 5510592011 Pipeline of Jenrin Discovery.
Ref 551296Morpholinoalkylindenes as antinociceptive agents: Novel cannabinoid receptor agonists, Bioorg. Med. Chem. Lett. 5(4):381-386 (1995).
Ref 551589Ghrelin agonist TZP-101/ulimorelin accelerates gastrointestinal recovery independently of opioid use and surgery type: covariate analysis of phase 2 data. World J Surg. 2012 Jan;36(1):39-45.
Ref 5517902011 Pipeline of Zydus Cadila Group.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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