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融合烟碱型乙酰胆碱受体的新旧观点。

Merging old and new perspectives on nicotinic acetylcholine receptors.

机构信息

Department of Pharmacology and Therapeutics, University of Florida, College of Medicine, PO Box 100267, 1200 Newell Drive, Gainesville, FL 32610-0267, USA.

出版信息

Biochem Pharmacol. 2014 May 1;89(1):1-11. doi: 10.1016/j.bcp.2014.01.029. Epub 2014 Jan 31.

Abstract

This review covers history underlying the discovery of the molecular mediators of nicotine's effects in the brain and the diversity of the nicotinic acetylcholine receptor (nAChR) subtypes. Models are presented for both their structure and their function as mediators of signal transduction, with special consideration of the differences between the two main subtypes: heteromeric receptors, which are specialized for rapid electrochemical signal transduction, and homomeric α7 receptors, which have come to be implicated in both ionotropic and metabotropic signaling. This review presents perspectives on the pharmacology and therapeutic targeting of nAChRs for the treatment of nicotine dependence or disease.

摘要

这篇综述涵盖了尼古丁在大脑中作用的分子介质的发现背后的历史,以及烟碱型乙酰胆碱受体(nAChR)亚型的多样性。本文提出了它们作为信号转导介质的结构和功能模型,特别考虑了两种主要亚型之间的差异:异源二聚体受体,专门用于快速电化学反应信号转导,以及同源 α7 受体,其涉及离子型和代谢型信号转导。本文就 nAChR 的药理学和治疗靶标提出了一些观点,以治疗尼古丁依赖或疾病。

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Merging old and new perspectives on nicotinic acetylcholine receptors.融合烟碱型乙酰胆碱受体的新旧观点。
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本文引用的文献

1
Stoichiometry for activation of neuronal α7 nicotinic receptors.神经元 α7 烟碱型乙酰胆碱受体激活的化学计量。
Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):20819-24. doi: 10.1073/pnas.1315775110. Epub 2013 Dec 2.
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Similar activity of mecamylamine stereoisomers in vitro and in vivo.美加明立体异构体在体外和体内的相似活性。
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