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Product Description
– 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].
Web ID
– HY-12206A
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C15H24N4S.xC4H4O4
References
– [1]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.|[2]J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.|[3]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.|[4]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.
CAS Number
– 148440-81-7
Molecular Weight
– N/A
SMILES
– S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3.O=C(O)/C=CC(O)=O.[x]
Clinical Information
– No Development Reported
Research Area
– Neurological Disease
Solubility
– 10 mM in DMSO
Target
– Histamine Receptor
Isoform
– H3 Receptor
Pathway
– GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling
Product type
– Reference compound
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