thioperamide

Thioperamide is a potent, selective, and blood-brain barrier-permeable antagonist and inverse agonist of the histamine H3 receptor (H3R). Originally characterized in the late 1980s, it serves as a prototypical pharmacological tool for studying the histaminergic system. By blocking H3 autoreceptors on histaminergic neurons, thioperamide prevents feedback inhibition, thereby increasing the synthesis and release of histamine in the central nervous system. It also acts on H3 heteroreceptors to modulate the release of other neurotransmitters, including acetylcholine, dopamine, and noradrenaline. Preclinical research has demonstrated that thioperamide can rescue circadian rhythm disruptions, improve memory consolidation (such as novel object recognition), and enhance wakefulness in animal models of neurodegenerative and sleep disorders, including Parkinson's disease and Alzheimer's disease.

Other names

thioperamide maleate