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α1和α6亚基可共存于同一小脑γ-氨基丁酸A型(GABAA)受体中,保持各自的苯二氮䓬结合特异性。

The alpha 1 and alpha 6 subunits can coexist in the same cerebellar GABAA receptor maintaining their individual benzodiazepine-binding specificities.

作者信息

Khan Z U, Gutiérrez A, De Blas A L

机构信息

Division of Molecular Biology and Biochemistry, School of Biological Sciences, University of Missouri-Kansas City 64110-2499, USA.

出版信息

J Neurochem. 1996 Feb;66(2):685-91. doi: 10.1046/j.1471-4159.1996.66020685.x.

DOI:10.1046/j.1471-4159.1996.66020685.x
PMID:8592140
Abstract

Two GABAA receptor subunit-specific antibodies anti-alpha 6 and anti-alpha 1 have been used for elucidating the relationship between the presence of alpha 1 and/or alpha 6 subunits in the cerebellar GABAA receptors and the benzodiazepine-binding specificity. Receptor immunoprecipitation with the subunit-specific antibodies shows that 39% of the cerebellar GABAA receptors have alpha 6, whereas 76% of the receptors have alpha 1 as determined by [3H]-muscimol binding. Results show that 42-45% of the receptors having alpha 6 also have alpha 1, whereas 13-15% of the receptors that contain alpha 1 also have alpha 6. The immunoprecipitation results as well as immunopurification and immunoblotting experiments reveal the existence of three types of cerebellar GABAA receptors; i.e., one has both alpha 1 and alpha 6 subunits, a second type has alpha 1 but not alpha 6, and a third type has alpha 6 but not alpha 1 subunits. The results also show that receptors where alpha 1 and alpha 6 subunits coexist have two pharmacologically different benzodiazepine-binding properties, each associated with a different alpha subunit. The alpha 1 subunit contributes the high-affinity binding of [3H]Ro 15-1788 (flumazenil) and the diazepam-sensitive binding of [3H]Ro 15-4513. The alpha 6 subunit contributes the diazepam-insensitive binding of [3H]Ro 15-4513, but it does not bind [3H]Ro 15-1788 with high affinity. Thus, in the cerebellar alpha 1- alpha 6 GABAA receptors, there is no dominance of the pharmacology of one alpha subunit over the other.

摘要

两种GABAA受体亚基特异性抗体,即抗α6和抗α1抗体,已被用于阐明小脑GABAA受体中α1和/或α6亚基的存在与苯二氮䓬结合特异性之间的关系。用亚基特异性抗体进行受体免疫沉淀显示,39%的小脑GABAA受体含有α6,而通过[3H] - 蝇蕈醇结合测定,76%的受体含有α1。结果表明,42 - 45%含有α6的受体也含有α1,而13 - 15%含有α1的受体也含有α6。免疫沉淀结果以及免疫纯化和免疫印迹实验揭示了三种类型的小脑GABAA受体的存在;即一种同时含有α1和α6亚基,第二种类型含有α1但不含有α6,第三种类型含有α6但不含有α1亚基。结果还表明,α1和α6亚基共存的受体具有两种药理学上不同的苯二氮䓬结合特性,每种特性与不同的α亚基相关。α1亚基促成了[3H]Ro 15 - 1788(氟马西尼)的高亲和力结合以及[3H]Ro 15 - 4513的地西泮敏感结合。α6亚基促成了[3H]Ro 15 - 4513的地西泮不敏感结合,但它不与[3H]Ro 15 - 1788高亲和力结合。因此,在小脑α1 - α6 GABAA受体中,一种α亚基的药理学特性并不占主导地位。

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