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组胺H3受体激动剂刺激的[35S]GTPγ[S]与百日咳毒素结合的敏感性。

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

作者信息

Clark E A, Hill S J

机构信息

Department of Physiology and Pharmacology, Queen's Medical Centre, Nottingham, UK.

出版信息

Eur J Pharmacol. 1996 Jan 25;296(2):223-5. doi: 10.1016/0014-2999(95)00800-4.

DOI:10.1016/0014-2999(95)00800-4
PMID:8838460
Abstract

The effect of histamine H3 receptor-selective ligands on [35S]guanosine 5'-o-(gamma-thio)triphosphate ([35S]GTP gamma[S]) binding has been examined in rat cerebral cortical membranes. R alpha-Methylhistamine and N alpha-methylhistamine produced a concentration-dependent stimulation of [35S]GTP gamma[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]GTP gamma[S]. These results provide the first evidence that histamine H3 receptors couple directly to a Gi/Go protein in mammalian brain.

摘要

在大鼠大脑皮层膜中研究了组胺H3受体选择性配体对[35S]鸟苷5'-O-(γ-硫代)三磷酸([35S]GTPγ[S])结合的影响。Rα-甲基组胺和Nα-甲基组胺对[35S]GTPγ[S]结合产生浓度依赖性刺激，在选择性组胺H3受体拮抗剂硫代哌啶存在下这种刺激减弱。此外，用百日咳毒素处理脑膜消除了组胺H3受体激动剂刺激的[35S]GTPγ[S]结合。这些结果提供了首个证据，表明组胺H3受体在哺乳动物大脑中直接与Gi/Go蛋白偶联。

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