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158681-13-1

中文名称 盐酸利莫那班
英文名称 Rimonabant hydrochloride
CAS 158681-13-1
分子式 C22H21Cl3N4O
MDL 编号 MFCD04034714
分子量 463.79
MOL 文件 158681-13-1.mol
更新日期 2023/03/20 15:41:23
158681-13-1 结构式 158681-13-1 结构式

基本信息

中文别名
5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺
5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺盐酸盐
利莫那班
盐酸利莫那班
5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺单盐酸盐
英文别名
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-n-1-piperidinyl-1h-pyrazole-3-carboxamide monohydrochloride
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-n-piperidinopyrazole-3-carboxamide
ACOMPLIA
RIMONABANT
RIMONABANT HYDROCHLORIDE
ACOMPLIA (RIMONABANT
RIMONABANT HCL
Rimonabant(Acomplia)
RimonabantConsultedStandard
Acomplia, SR141716
SR 141716A
5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide monohydrochloride
所属类别
医药中间体:原料药中间体

物理化学性质

熔点230-240°C
储存条件2-8°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

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301-H319
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 Germany3

常见问题列表

概述
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。
生物活性
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)。
靶点

CB1

1.8 nM (Ki)

体外研究

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%.

体内研究

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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