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Thioperamide maleate
Chemical Name:N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioami
de maleate
Biological Activity:
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.
Hew et al (1990) Characterisation of histamine H3 receptors in guinea pig
ileum with H3 selective ligands. Br.J.Pharmacol. 101 621. Liu
et al (2001) Cloning and pharmacological characterization of a fourth
histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59
420. Linget al (2004) Histamine H4 receptor mediates
eosinophil chemotaxis with cell shape change and adhesion molecule
upregulation. Br.J.Pharmacol. 142 161. Gbahouet al
(2006) Compared pharmacology of human H3 and H4
receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol.
147 744.
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This accurate purity data is available on a batch-specific basis for every product via our website. At Tocris we work hard to ensure that we always supply to the highest possible standards of purity.
