同义名 :	SR 141716A Hydrochloride; Rimonabant Hydrochloride; Rimonabant(Hydrochloride)
	CAS号 :	158681-13-1
	货号 :	A327195
	分子式 :	C22H22Cl4N4O
	纯度 :	98%
	分子量 :	500.25
	MDL号 :	MFCD00934884
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Rimonabant HCl is a hydrochloride form of Rimonabant. Rimonabant is a first selective oral antagonist of CB1 (cannabinoid receptor 1), which belongs to the guanine-nucleotide-binding protein (G-protein) coupled receptor family. In CB1 transfected HEK293 cells, the IC50 concentration of rimonabant was 13.6 nM and the EC50 concentration was 17.3 nM. Rimonabant was famous for its potent anorectic anti-obesity ability for decades and has been demonstrated to effectively reduce body weight by inducing a reduction in appetite. It also benefits for lowing cardiovascular metabolic risk events. However, it was withdrawn because of the severe byproduct in 2009, especially depression and anxiety. Mechanically, rimonabant promotes adenylate cyclase activity in a dose-dependent, stereoselective and pertussis toxin-sensitive manner by directly targeting to CB1. In vitro, rimonabant dose-dependently reduced ACAT activity in Raw264.7 macrophages and isolated peritoneal macrophages with an IC50 of 2.9 μM. Rimonabant also inhibited ACAT activity in CHO-ACAT1 and CHO-ACAT2 cells with an IC50 of 1.5 μM and 2.2 μM respectively. Rimonabant treatment blocks ACAT-related processes in macrophages, including oxysterol-induced apoptosis, and acetylated LDL-induced foam cell formation. Rimonabant was able to alter the cell cycle distribution in almost all type of cell lines and then significantly reduces cell growth and induces death in human colorectal cancer cells (DLD-1, CaCo-2 and SW620). However, rimonabant causes cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis. In vivo, Rimonabant significantly reduced the formation of abnormal crypt foci (ACF) before colorectal cancer formation in the oxidative azomethane-induced colon cancer model. In the experiment of long-term rimonabant treated obese Zucker rats, platelet-bound fibrinogen, serum levels of RANTES (normal T cell expression and secretion of regulatory proteins) and MCP-1 (monocyte chemoattractant protein-1) were decreased to the levels observed in lean Zucker rats.

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.00mL 0.40mL 0.20mL	10.00mL 2.00mL 1.00mL	19.99mL 4.00mL 2.00mL

参考文献
[1]Esposito I, Proto MC, et al. The cannabinoid CB1 receptor antagonist rimonabant stimulates 2-deoxyglucose uptake in skeletal muscle cells by regulating the expression of phosphatidylinositol-3-kinase. Mol Pharmacol. 2008 Dec;74(6):1678-86. [2]Molecule of the month. Rimonabant hydrochloride. Drug News Perspect. 2004 Jul-Aug;17(6):403.