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158681-13-1

中文名稱(chēng) 鹽酸利莫那班
英文名稱(chēng) Rimonabant hydrochloride
CAS 158681-13-1
分子式 C22H21Cl3N4O
MDL 編號(hào) MFCD04034714
分子量 463.79
MOL 文件 158681-13-1.mol
更新日期 2024/06/03 14:41:39
158681-13-1 結(jié)構(gòu)式 158681-13-1 結(jié)構(gòu)式

基本信息

中文別名
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-甲酰胺鹽酸鹽
利莫那班
鹽酸利莫那班
5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺單鹽酸鹽
英文別名
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
所屬類(lèi)別
醫(yī)藥中間體:原料藥中間體

物理化學(xué)性質(zhì)

熔點(diǎn)230-240°C
儲(chǔ)存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
形態(tài)粉末
顏色白色至米色
CAS 數(shù)據(jù)庫(kù)158681-13-1(CAS DataBase Reference)

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301-H319
危險(xiǎn)品標(biāo)志T,Xi
危險(xiǎn)類(lèi)別碼25-36
安全說(shuō)明26-45
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1 / PGIII
WGK Germany3

常見(jiàn)問(wèn)題列表

概述
鹽酸利莫那班是一種大麻素受體-1(CB1)拈抗劑, 通過(guò)阻斷腦組織中的大麻素受體來(lái)降低人的食欲和煙癮,可用于肥胖、煙癮、高血壓、血脂異常和2-型糖尿病和代謝綜合癥的治療,同時(shí)可以降低膽固醇,具有預(yù)防肥胖人群患上心臟病和糖尿病的功效,已于2006年在多個(gè)國(guó)家上市。
生物活性
Rimonabant hHydrochloride (SR 141716A Hydrochloride) 是中心大麻素受體 1 (CB1) 高效的、選擇性的反向激動(dòng)劑, Ki 值為1.8 nM。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 也能夠抑制分枝桿菌膜蛋白3 (MMPL3)。
靶點(diǎn)

CB1

1.8 nM (Ki)

體外研究

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%.

體內(nèi)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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