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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
H3 Receptor
Available Sizes
Frequently Asked Questions
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