Thioperamide is a potent HRH₄ antagonist and selective HRH₃

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

capable of crossing the

blood–brain barrier The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that prevents solutes in the circulating blood from ''non-selectively'' crossing into the extracellular fluid of ...

. It was used by

Jean-Charles Schwartz Jean-Charles Schwartz, born on May 28, 1936, in Paris, is a French neurobiologist, pharmacist and researcher. Husband of Ketty Schwartz, née Gersen (1937-2007) and father of Olivier, Marc and Emmanuelle. He is a member of the Academy of Sciences.. ...

in his early experiments regarding the H₃ receptor. Thioperamide was found to be an antagonist of histamine

autoreceptor An autoreceptor is a type of receptor located in the membranes of nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or hormones released by the neuron on which the aut ...

s, which negatively regulate the release of histamine, and enhances the activity of histaminergic neurons by blocking autoreceptors, leading to greater release of histamine. Its action on H₃ is thought to promote wakefulness and improve memory consolidation.

References

H3 receptor antagonists Thioureas Piperidines Imidazoles Cyclohexyl compounds {{nervous-system-drug-stub

See also

References