Tags: Drug.

Thioperamide is a potent HRH4 antagonist and selective HRH3 antagonist that is capable of crossing the blood–brain barrier.Thioperamide was used by Jean-Charles Schwartz in his early experiments regarding the H3 receptor. Thioperamide was found to be an antagonist of histamine autoreceptors which negatively regulate the release of histamine; thioperamide enhances the activity of histaminergic neurons by blocking autoreceptors leading to greater release of histamine.

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