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

https://doi.org/10.1016/0014-2999(95)00800-4Get rights and content

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.

References (11)

There are more references available in the full text version of this article.

Cited by (93)

  • Histaminergic effects on the frequency of repetitive spike firing in rat insular cortex

    2012, Neuroscience Letters
    Citation Excerpt :

    Intracellular recordings using slice preparations demonstrate that H2 receptors, coupling to Gs protein, increase the frequency of repetitive spike firing of cortical neurons by blocking Ca2+-dependent K+ channels that regulate afterhyperpolarization (AHP) [12,13]. In contrast to the studies of H2 receptors in the cerebral cortex, little information is available regarding the functional roles of H3 receptors [16], which decrease cyclic-3′,5′-adenosine monophosphate (cAMP) concentration and Ca2+ conductance by activating Gi/o protein [3] and regulate neural firing, histamine synthesis and release of histamine as autoreceptors [6,15,19,21]. Taking into account the finding that H3 receptors are highly expressed in the cerebral cortex [4,11,16], there is a possibility that H3 receptors affect neural functions, including the action potential properties in the IC.

View all citing articles on Scopus
View full text