Thioperamide (maleate)

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

Product Specifications

CAS Number

[148440-81-7]

Product Name Alternative

MR-12842 (maleate)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/thioperamide-maleate.html

Purity

98.26

Solubility

H2O : 100 mg/mL (ultrasonic)

Smiles

S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3.O=C(O)/C=C\C(O)=O.[x]

Molecular Formula

C15H24N4S.xC4H4O4

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[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.