Thioperamide maleate  (Synonyms: MR-12842 maleate)

Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [³H]histamine release. Thioperamide maleate inhibits [³H]histamine synthesis with a K_i of 31 nM^[1].

Thioperamide inhibits [³H]-(R)α-MeHA binding rat brain and guinea-pig lung with K_is of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [³H]histamine release with a mean apparent K_i 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 (K_i=43 and 60 nM, respectively)^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

C₁₅H₂₄N₄S.xC₄H₄O₄

148440-81-7

固体

White to off-white

硫丙咪胺马来酸

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]