title: Interaction of clozapine with the histamine H3 receptor in rat brain.
abstract: We examined possible interactions between neuroleptics and the histamine H3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H3 antagonist, [125I]-iodophenpropit, we observed a Ki of 236 +/- 87 nM. Functionally, clozapine was studied on the H3-mediated inhibition of [3H]-5-hydroxytryptamine ([3H]-5-HT) release from rat brain cortex slices. Clozapine acts as an antagonist with an apparent KB value of 79.5 nM.
authors.affiliation: Department of Pharmacology, Mount Sinai School of Medicine of the City University of New York, N.Y. 10029, USA.
authors.forename: A A
authors.initials: AA
authors.lastname: Rodrigues
authors.forename: F P
authors.initials: FP
authors.lastname: Jansen
authors.forename: R
authors.initials: R
authors.lastname: Leurs
authors.forename: H
authors.initials: H
authors.lastname: Timmerman
authors.forename: G D
authors.initials: GD
authors.lastname: Prell
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D003024:Clozapine / Q000494:pharmacology*; D006220:Haloperidol / Q000494:pharmacology; D006633:Histamine Antagonists; D006636:Histamine Release / Q000187:drug effects; D007093:Imidazoles / Q000494:pharmacology; D007550:Isothiuronium / Q000031:analogs & derivatives / Q000494:pharmacology; D008761:Methylhistamines / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000378:metabolism
chemical_list: D006633:Histamine Antagonists; D007093:Imidazoles; D008761:Methylhistamines; D010880:Piperidines; D018100:Receptors, Histamine H3; D007550:Isothiuronium; C077791:iodophenpropit; C069357:alpha-methylhistamine; C052075:thioperamide; D003024:Clozapine; D006220:Haloperidol