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在小鼠成纤维细胞中稳定表达的主要脑烟碱型乙酰胆碱受体亚型的结构和药理学特性

Structural and pharmacological characterization of the major brain nicotinic acetylcholine receptor subtype stably expressed in mouse fibroblasts.

作者信息

Whiting P, Schoepfer R, Lindstrom J, Priestley T

机构信息

Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Harlow, Essex, UK.

出版信息

Mol Pharmacol. 1991 Oct;40(4):463-72.

PMID:1717818
Abstract

Previously, we purified the predominant subtype of brain nicotinic acetylcholine receptor (AChR), analyzed its structure, and found that it was composed of two kinds of subunit, with sequences encoded by cDNAs termed alpha 4 and beta 2. Here we express these cDNAs from chicken brain in stably transfected fibroblasts. We demonstrate by synthesis that these cDNAs encode subunit polypeptides of the expected sizes, which coassemble to form receptor macromolecules having the same size as native AChRs. Additionally, we demonstrate that the expressed AChRs exhibit the ligand-binding pharmacology of native brain AChRs and function as acetylcholine-gated ion channels.

摘要

此前,我们纯化了脑烟碱型乙酰胆碱受体(AChR)的主要亚型,分析了其结构,发现它由两种亚基组成,其序列由称为α4和β2的cDNA编码。在此,我们在稳定转染的成纤维细胞中表达来自鸡脑的这些cDNA。我们通过合成证明这些cDNA编码预期大小的亚基多肽,它们共同组装形成与天然AChR大小相同的受体大分子。此外,我们证明所表达的AChR表现出天然脑AChR的配体结合药理学特性,并作为乙酰胆碱门控离子通道发挥作用。

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Structural and pharmacological characterization of the major brain nicotinic acetylcholine receptor subtype stably expressed in mouse fibroblasts.在小鼠成纤维细胞中稳定表达的主要脑烟碱型乙酰胆碱受体亚型的结构和药理学特性
Mol Pharmacol. 1991 Oct;40(4):463-72.
2
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