Thioperamide maleate is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro with a pKi value of 8.4 and inhibits histamine binding in vivo with an ED50 value of 1 mg/kg.1 At a dose of 5 mg/kg thioperamide maleate inhibits kindled seizures in rats by decreasing histamine and gamma-aminobutyric acid.2
1
Meir, G., Apelt, J., Reichert, U., et al. Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists. Eur J Pharm Sci13249-259(2001).
2
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).
Thurmond, R.L., Gelfand, E.W., and Dunford, P.J. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov741-53(2008).
Size
Price
Quantity
Subtotal
1 mg
$10.00
$0.00
5 mg
$45.00
$0.00
10 mg
$80.00
$0.00
25 mg
$175.00
$0.00
Bulk
Contact
Cart Total
$0.00
This product is available in custom sizes and/or larger quantities.