Thioperamide
Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
Purity: ≥99%
Biological Activity
Thioperamide is a potent histamine H3 and H4 antagonist/inverse agonist. Ki values are 25 and 27 nM for human recombinant H3 and H4 receptors respectively. Blocks eosinophil shape change (IC50 = 1.4 μM) and chemotaxis (IC50 = 519 nM) induced by histamine. Freely crosses the blood-brain barrier.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Gbahou et al.
Br.J.Pharmacol., 2006;147:744 -
Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands.
Hew et al.
Br.J.Pharmacol., 1990;101:621 -
Characterisation of histamine H3 receptors in guinea pig ileum with H3 selective ligands.
Hew et al.
Br.J.Pharmacol., 1990;101:621 -
Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation.
Ling et al.
Br.J.Pharmacol., 2004;142:161 -
Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow.
Liu et al.
Mol. Pharmacol., 2001;59:420
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Citations for Thioperamide
The citations listed below are publications that use Tocris products. Selected citations for Thioperamide include:
4 Citations: Showing 1 - 4
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Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma.
Authors: Francis Et al.
Gut 2012;61:753
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Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells.
Authors: Holden Et al.
Saudi J Biol Sci 2007;152:891
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Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype.
Authors: Takahashi Et al.
J Clin Invest 2002;110:1791
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Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells.
Authors: Robinson and Dickenson
Br J Pharmacol 2001;133:1378
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