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Thioperamide(maleate)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Thioperamide(maleate)图片
CAS NO:148440-81-7
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Thioperamide (maleate) (MR-12842 maleate) 是一种有效的、可口服的、脑渗透剂和选择性 H3 受体拮抗剂，Ki 为 4.3 nM，用于抑制 [3H] 组胺的释放。
Cas No.148440-81-7
别名硫丙咪胺马来酸,MR-12842 maleate
化学名N-cyclohexyl-4-(1H-imidazol-5-yl)-1-piperidinecarbothioamide, 2Z-butenedioate
Canonical SMILESS=C(NC1CCCCC1)N(CC2)CCC2C3=CN=CN3.O=C(/C=C\C(O)=O)O
分子式C15H24N4S•C4H4O4
分子量408.5
溶解度10mg/mL in ethanol, 25mg/mL in DMSO, 30mg/mL in DMF
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Thioperamide (maleate) is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro with a pKi value of 8.4 and inhibits histamine binding in vivo with an ED50 value of 1 mg/kg.[1] At a dose of 5 mg/kg thioperamide (maleate) inhibits kindled seizures in rats by decreasing histamine and gamma-aminobutyric acid.[2]

Reference:
[1]. Meir, G., Apelt, J., Reichert, U., et al. Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists. European Journal of Pharmaceutical Sciences 13, 249-259 (2001).
[2]. Harada, C., Fujii, Y., Hirai, T., et al. Inhibitory effect of iodophenprofit, a selective histamine H3 antagonist, on amygdaloid kindled seizures. Brain Research Bulletin 63, 143-146 (2004).