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.
MeSH terms
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Animals
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Binding, Competitive
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Cerebral Cortex / drug effects*
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Cerebral Cortex / metabolism
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Clozapine / pharmacology*
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Haloperidol / pharmacology
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Histamine Antagonists
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Histamine Release / drug effects
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Imidazoles / pharmacology
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Isothiuronium / analogs & derivatives
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Isothiuronium / pharmacology
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Methylhistamines / pharmacology
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Piperidines / pharmacology
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Rats
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Receptors, Histamine H3 / drug effects*
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Receptors, Histamine H3 / metabolism
Substances
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Histamine Antagonists
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Imidazoles
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Methylhistamines
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Piperidines
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Receptors, Histamine H3
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Isothiuronium
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iodophenpropit
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alpha-methylhistamine
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thioperamide
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Clozapine
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Haloperidol