1019839-52-1

1019839-52-1 structure

Name: CB1 inverse agonist 2
Chemical Name: N-Butyl-11-(3-chloro-4-fluorophenyl)dibenzo[b,f][1,4]thiazepine-8 -carboxamide
CAS Number: 1019839-52-1
Molecular Formula: C₂₄H₂₀ClFN₂OS
Molecular Weight: 438.94500
Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
Create Date: 2017-06-16 19:24:24
Modify Date: 2024-01-06 16:08:22
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].

Name	N-Butyl-11-(3-chloro-4-fluorophenyl)dibenzo[b,f][1,4]thiazepine-8 -carboxamide

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor
Target	CB1:9.7 (pKi) CB2:6.0 (pKi)
In Vitro	CB1 inverse agonist 2 (compound 12 h) 对 CB1 具有选择性，对 CB1 和 CB2 的 pKi 值分别为 9.7 和 6.0[1]。
In Vivo	CB1 inverse agonist 2 (compound 12 h) (1 mg/kg; 腹腔注射; 单次剂量) 对体温降低的抑制程度达到 70%，(10mg /kg;口服; 单剂量) 对食物摄入的抑制率达到 59%[1]。 CB1 inverse agonist 2 (10 mg/kg; 口服; 每天一次，持续 14 天) 导致小鼠体重与初始体重相比，出现 13% 的减轻[1]。
References	[1]. Synthesis and Evaluation of Dibenzothiazepines: A Novel Class of Selective Cannabinoid-1 Receptor Inverse AgonistsJ. 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.