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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.