烟碱乙酰胆碱受体作为药物靶点。

R C Hogg, D Bertrand
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引用次数: 106

摘要

虽然长期以来一直有文献记载烟叶中所含的尼古丁会引起重大的公共健康问题,但也有人观察到这种生物碱可以产生有益的影响。然而,随着神经元烟碱乙酰胆碱受体编码基因家族的鉴定,以及对其在中枢神经系统中的表达和功能的了解的增加,这些受体才开始关注其作为药物靶点的潜力。鉴于有关烟碱乙酰胆碱受体及其参与疾病状态的最新发现,我们回顾了设计针对这些配体门控通道的新药的可能性。我们讨论了激动剂、拮抗剂和变构调节剂的有益和可能的不良作用,并从我们最新知识的角度进行了讨论。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Nicotinic acetylcholine receptors as drug targets.

While it has long been documented that nicotine contained in tobacco leaves gives rise to major public health problems it has also been observed that this alkaloid can have beneficial effects. However, it is only with the identification of a family of genes coding for the neuronal nicotinic acetylcholine receptors and increased knowledge of their expression and function in the central nervous system that these receptors have received attention concerning their potential as drug targets. In light of the latest findings about nicotinic acetylcholine receptors and their involvement in disease states we review the possibility to design new drugs targeted to these ligand-gated channels. Beneficial and possible undesirable actions of agonists, antagonists and allosteric modulators are discussed and placed in perspective of our most recent knowledge.

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