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牛肾上腺髓质中的毒蕈碱受体亚型

Muscarinic receptor subtypes in bovine adrenal medulla.

作者信息

Aguilar J S, Ballesta J J, Reig J A, Palmero M, Viniegra S, Criado M

机构信息

Departamento de Neuroquímica, Universidad de Alicante, Spain.

出版信息

Neurochem Res. 1992 Dec;17(12):1235-9. doi: 10.1007/BF00968406.

Abstract

Catecholamine secretion in the bovine adrenal medulla is evoked largely by nicotinic receptor activation. However, bovine adrenal medulla also contain muscarinic receptors that mediate several cell responses. To understand the physiological role of muscarinic receptors in the bovine adrenal medulla it is important to identify the pharmacological subtypes present in this tissue. For this, we analyzed the abilities of different selective muscarinic antagonists in displacing the binding of the non-selective antagonist [3H] quinuclidinyl benzylate to an enriched plasma membrane fraction prepared from bovine adrenal medulla. All the selective antagonists bind at least two bindings sites with different affinities. The binding profile of the sites with high proportion is similar to the M2 subtype and those present in low proportion have a M1 profile. However, some variation in the proportion of the sites for the different ligands suggest the presence of the third pharmacological subtype (M3). We conclude that the sites in high proportion (60-80%) correspond to M2 muscarinic subtypes, and the rest is constituted by M1 plus M3 subtypes. The presence of multiplicity of subtypes in the adrenal medulla membranes suggests a diversity of functions of muscarinic receptors in the adrenal gland.

摘要

牛肾上腺髓质中的儿茶酚胺分泌主要由烟碱样受体激活引起。然而,牛肾上腺髓质也含有介导多种细胞反应的毒蕈碱样受体。为了解毒蕈碱样受体在牛肾上腺髓质中的生理作用,识别该组织中存在的药理学亚型很重要。为此,我们分析了不同选择性毒蕈碱拮抗剂置换非选择性拮抗剂[3H]喹核醇基苯甲酸酯与从牛肾上腺髓质制备的富集质膜部分结合的能力。所有选择性拮抗剂都以不同亲和力结合至少两个结合位点。高比例位点的结合特征与M2亚型相似,低比例位点的结合特征与M1亚型相似。然而,不同配体位点比例的一些变化表明存在第三种药理学亚型(M3)。我们得出结论,高比例(60-80%)的位点对应于M2毒蕈碱亚型,其余由M1加M3亚型组成。肾上腺髓质膜中多种亚型的存在表明肾上腺中毒蕈碱样受体功能的多样性。

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