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Thioperamide maleate

MCE 国际站：Thioperamide maleate

品牌：MedChemExpress (MCE)

货号：HY-12206A

CAS 号：148440-81⁻⁷

生物活性：马来酸硫哌酰胺（MR-12842 马来酸盐）是一种强效、口服有效、可穿透血脑屏障的选择性 H3 受体拮抗剂，对 [3H]组胺释放的抑制 Ki 值为 4.3 nM。马来酸硫哌酰胺对 [3H]组胺合成的抑制 Ki 值为 31 nM[1]。

体外研究(In Vitro)：Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM[1]. Thioperamide (0.01-100 µM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner[2]. Thioperamide displays similar potencies at human H4 and H3 receptors (Ki=43 and 60 nM, respectively)[3]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice[4]. MCE尚未独立确认这些方法的准确性。 仅供参考。

Formula：C15H24N4S.xC4H4O4

性状：固体

颜色：White to off-white

中文名称：硫丙咪胺马来酸

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式： 4°C，密封保存，避免受潮 *溶剂保存：-80°C，6个月；-20°C，1个月（密封保存，避免受潮）

文献引用：MCE 顾客使用本产品发表 3 篇科研文献

提供质量检测报告：Data Sheet、SDS、COA、HNMR、RP-HPLC、MS、产品使用指南

产品活性：Thioperamide maleate (MR-12842 maleate) 是一种有效的，具有口服活性的，可透过血脑屏障的选择性 H3 受体拮抗剂，抑制 [3H] 组胺释放的Ki 为 4.3 nM。Thioperamide maleate 抑制 [3H] 组胺合成的 Ki 为 31 nM 。

相关产品：(R)-(-)-α-Methylhistamine dihydrochloride | Mepyramine maleate | Ranitidine hydrochloride | RSL3 | CH-223191 | A-967079 | Mepyramine maleate (Standard) | Omaveloxolone | SAR7334 hydrochloride | RSL3 (Standard) | Ranitidine hydrochloride (Standard) | A-967079 (Standard)

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

参考文献：
[1]. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.
[2]. Na Wang, et al. Histamine H3 Receptor Antagonist Enhances Neurogenesis and Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairments. Front Pharmacol. 2020 Jan 21;10:1583.
[3]. Y Charlier, et al. Differential Effects of Histamine H(3) Receptor Inverse Agonist Thioperamide, Given Alone or in Combination With the N-methyl-d-aspartate Receptor Antagonist Dizocilpine, on Reconsolidation and Consolidation of a Contextual Fear Memory in Mice. Neuroscience. 2011 Oct 13;193:132-42.
[4]. Gbahou F, et al. Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol. 2006;147(7):744⁻⁷54.