148440-81-7

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 pK_i value of 8.4 and inhibits histamine binding in vivo with an ED₅₀ value of 1 mg/kg. At a dose of 5 mg/kg thioperamide (maleate) inhibits kindled seizures in rats by decreasing histamine and gamma-aminobutyric acid.

Thioperamide maleate salt was used to study the sympathetic and autonomic nerve activity in mammalian white adipose tissue.

Thioperamide is a potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier. It affects the central histaminergic system and decreases the duration of seizures and convulsions in mice. It also improves learning deficit induced by other drugs such as scopolamine.

H₃ Receptor

[1] GALINA MEIER . Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists[J]. European Journal of Pharmaceutical Sciences, 2001, 13 3: Pages 249-259. DOI: 10.1016/s0928-0987(01)00106-3
[2] CHIE HARADA. Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures[J]. Brain Research Bulletin, 2004, 63 2: Pages 143-146. DOI: 10.1016/j.brainresbull.2004.02.001