Thioperamide

Thioperamide (MR-12842) 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 inhibits [3H]histamine synthesis with a Ki of 31 nM[1].

Product Specifications

CAS Number

[106243-16-7]

Product Name Alternative

MR-12842

UNSPSC

12352005

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.html

Concentration

10mM

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C15H24N4S

Molecular Weight

292.44

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.