Thioperamide  (Synonyms: MR-12842)

Thioperamide (MR-12842) 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 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].

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^[3].

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

292.44

C₁₅H₂₄N₄S

106243-16-7

S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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  [Content Brief]