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Clobenpropit dihydrobromide
Other Information:
Sold with the permission of SCI, Amsterdam
Chemical Name:N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothio
urea dihydrobromide
Biological Activity:
An extremely potent histamine H3
antagonist/inverse agonist (pA2=9.93). Also displays partial agonist
activity at H4 receptors; induces eosinophil shape change with an EC50
of 3 nM.
Van der Goot et al (1992) Isothiourea analogues of
histamine as potent agonists or antagonists of the histamine H3
receptor. Eur.J.Med.Chem. 27 511. Yokoyama et al (1994)
Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist,
inhibits electrically induced convulsions in mice. Eur.J.Pharmacol. 260 23.
Liu et al (2001) Cloning and pharmacological characterization of
a fourth histamine receptor (H4) expressed in bone marrow. Mol.
Pharmacol. 59 420. Bucklandet al (2003) Histamine
induces cytoskeletal changes in human eosinophils via the H4 receptor.
Br.J.Pharmacol. 140 1117.
