Interaction of clozapine with the histamine H3 receptor in rat brain

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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.