Antagonism of central histamine H1 receptors by antipsychotic drugs.
The activity of 8 widely antipsychotic drugs as antagonists of central histamine H1 receptors was determined from the inhibition of the binding of 3H-mepyramine to a membrane fraction from guinea-pig brain. The phenothiazines examined, clorpromazine, fluphenazine, thioridazine and trifluoperazine, were all potent H1 antagonists. Both alpha- and beta-flupenthixol were potent inhibitors, but butaclamol, although less potent, showed stereospecificity. Haloperidol and spiperone were markedly weaker antihistamines than the phenothiazines.
D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists; D066298:In Vitro Techniques; D007700:Kinetics; D011738:Pyrilamine / Q000378:metabolism
D014150:Antipsychotic Agents; D006634:Histamine H1 Antagonists; D011738:Pyrilamine