CB1 inverse agonist 2

Modify Date: 2025-08-31 17:05:33

CB1 inverse agonist 2 Structure
CB1 inverse agonist 2 structure
 Common Name CB1 inverse agonist 2
CAS Number 1019839-52-1 Molecular Weight 438.94500
Density N/A Boiling Point N/A
Molecular Formula C24H20ClFN2OS Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CB1 inverse agonist 2


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].

 Names

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

 CB1 inverse agonist 2 Biological Activity

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
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.  

 Chemical & Physical Properties

Molecular Formula C24H20ClFN2OS
Molecular Weight 438.94500
Exact Mass 438.09700
PSA 70.25000
LogP 6.65310
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