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Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTPγ[S]binding to pertussis toxin

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Abstract

The effect of histamine H3 receptor-selective ligands on [35S]guanosine 5′-o-(γ-thio)triphosphate ([35S]GTPγ[S]) binding has been examined in rat cerebral cortical membranes. Rα-Methylhistamine and Nα-methylhistamine produced a concentration-dependent stimulation of [35S]GTPγ[S]binding which was attenuated in the presence of the selective histamine H3 receptor antagonist thioperamide. In addition, treatment of brain membranes with pertussis toxin abolished the histamine H3 receptor agonist stimulated binding of [35S]GTPγ [S]. These results provide the first evidence that histamine H3 receptors couple directly to a Gi/Go protein in mammalian brain.

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