CB1 inverse agonist 2

Names

[ CAS No. ]:
1019839-52-1

[ Name ]:
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]:

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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C24H20ClFN2OS

[ Molecular Weight ]:
438.94500

[ Exact Mass ]:
438.09700

[ PSA ]:
70.25000

[ LogP ]:
6.65310

Related Compounds