Thioperamide maleate 是一种有效且选择性的 H3 受体拮抗剂 (Ki = 4.3 nM),可抑制 [3H]histamine 的合成 (Ki = 31 nM)。
产品描述
Thioperamide maleate is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM).
体外活性
Thioperamide maleate (0.01, 0.1, 1, 10, 100 μM) promotes the viability of NE-4C stem cells in a concentration-dependent manner[1]. Thioperamide maleate displays similar potencies at human H4 and H3 receptors with Kis of 43 and 60 nM, respectively[2]. Thioperamide maleate inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide maleate competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM[4].
体内活性
In C57BL/6J mice, Thioperamide (5-20 mg/kg; i.p.) facilitates reconsolidation of a contextually-conditioned fear memory[3].
Cas No.
148440-81-7
分子式
C19H28N4O4S
分子量
408.52
别名
MR-12842 maleate;硫丙咪胺马来酸
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years