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盐酸利莫那班
产品纠错
CAS号:158681-13-1 | 英文名称:Rimonabant hydrochloride
分子式 C22H21Cl3N4O.ClH
分子量 500
EINECS号 233-720-0
MDL MFCD00934884
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 盐酸利莫那班
英文名称 Rimonabant hydrochloride
CAS号 158681-13-1
分子式 C22H21Cl3N4O.ClH
分子量 500.25
EINECS号 233-720-0
物化性质
熔点 230-240°C
溶解度 在DMSO中的溶解度为20mg/mL,澄清
形态 粉末
颜色 白色至米色
安全信息
危险品标志 T,Xi
危险类别码 25-36
安全说明 26-45
危险品运输编号 UN 2811 6.1 / PGIII
WGK Germany 3
生产及用途
盐酸利莫那班是一种大麻素受体-1(CB1)拈抗剂, 通过阻断脑组织中的大麻素受体来降低人的食欲和烟瘾,可用于肥胖、烟瘾、高血压、血脂异常和2-型糖尿病和代谢综合症的治疗,同时可以降低胆固醇,具有预防肥胖人群患上心脏病和糖尿病的功效,已于2006年在多个国家上市。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 是中心大麻素受体 1 (CB1) 高效的、选择性的反向激动剂, Ki 值为1.8 nM。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 也能够抑制分枝杆菌膜蛋白3 (MMPL3)。

CB1

1.8 nM (Ki)

Rimonabant could inhibit the growth of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is the direct target of rimonabant.
Rimonabant itself (10 -12 -10 -3 M, 12 concentrations) inhibits the basal binding of [ 35 S]GTPgS to human cortical membranes in a concentration dependent manner, with a -log IC 50 of 4.7±0.2 (IC 50 = 20 μM) and a maximal inhibition of 48±2%.

Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES and MCP-1 serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant .
Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors.

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