Clobenpropit dihydrobromide is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier; inhibits histamine binding in rat brain with an ED50 value of 10.5 mg/kg; protects cultured cortical neurons from NMDA-induced excitotoxicity by stimulating GABA release; in mice and rats protects against kindled seizures through its effects on histamine and GABA.
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N=C(SCCCc1cnc[nH]1)NCc1ccc(Cl)cc1
Background Reading
Barnes, J.C., Brown, J.D., Clarke, N.P., et al. Pharmacological activity of VUF 9153, an isothiourea histamine H3 receptor antagonist. Eur J Pharmacol250147-152(1993).
Harada, C., Fujii, Y., Hirai, T., et al. Inhibitory effect of iodophenprofit, a selective histamine H3 antagonist, on amygdaloid kindled seizures. Brain Res Bull63143-146(2004).
Dai, H., Fu, Q., Shen, Y., et al. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur J Pharmacol563117-123(2007).
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