| Identification | Back Directory | [Name]
Dibenzo[b,f][1,4]thiazepine-8-carboxaMide, N-butyl-11-(3-chloro-4-fluorophenyl)- | [CAS]
1019839-52-1 | [Synonyms]
CB1 inverse agonist 2
N-butyl-6-(3-chloro-4-fluorophenyl)benzo[b][1,4]benzothiazepine-3-carboxamide
Dibenzo[b,f][1,4]thiazepine-8-carboxaMide, N-butyl-11-(3-chloro-4-fluorophenyl)- | [Molecular Formula]
C24H20ClFN2OS | [MOL File]
1019839-52-1.mol | [Molecular Weight]
438.945 |
| Hazard Information | Back Directory | [Uses]
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model[1]. | [in vivo]
CB1 inverse agonist 2 (compound 12 h) (1 mg/kg; i.p.; single dose) results 70% inhibition against hypothermia, as well as (10 mg/kg; p.o.; single dose) resulting 59% inhibition against food intake[1].
CB1 inverse agonist 2 (10 mg/kg; p.o.; once daily for 14 d) produces robust weight loss of approximately 13% of initial body weight in mouse[1].
| [IC 50]
CB1: 9.7 (pKi); CB2: 6.0 (pKi) | [References]
[1] Synthesis and Evaluation of Dibenzothiazepines: A Novel Class of Selective Cannabinoid-1 Receptor Inverse Agonists
J. Med. Chem., 2009, 52 (7), pp 1975-1982
[2] Pettersson H, et al. Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. J Med Chem. 2009 Apr 9;52(7):1975-82. DOI:10.1021/jm801534c |
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