Cat. No. 0644
Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-pi
Biological ActivityPotent 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. Also available as part of the Histamine H3 Receptor Tocriset™.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Gbahou et al (2006) Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol. 147 744. PMID: 16432504.
Ling et al (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br.J.Pharmacol. 142 161. PMID: 15131002.
Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420. PMID: 11179434.
Hew et al (1990) Characterisation of histamine H3 receptors in guinea pig ileum with H3 selective ligands. Br.J.Pharmacol. 101 621. PMID: 1963802.
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Citations are publications that use Tocris products. Selected citations for Thioperamide include:
Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753. PMID: 21873469.
Holden et al (2007) Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells. Saudi J Biol Sci 152 891. PMID: 17891168.
Takahashi et al (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110 1791. PMID: 12488429.
Robinson and Dickenson (2001) Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells. Br J Pharmacol 133 1378. PMID: 11498525.
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Keywords: Thioperamide, supplier, H4, inverse, agonists, H3, antagonists, Receptors, Histamine, histaminergic, Tocris Bioscience, Histamine H3 Receptor Antagonist products