Laboratory of Neurobiology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, NC 27709, USA.
Biochem Pharmacol. 2011 Oct 15;82(8):952-8. doi: 10.1016/j.bcp.2011.04.020. Epub 2011 May 7.
Nicotinic acetylcholine receptors are ligand-gated ion conducting transmembrane channels from the Cys-loop receptor super-family. The α4β2 subtype is the predominant heteromeric subtype of nicotinic receptors found in the brain. Allosteric modulators for α4β2 receptors interact at a site other than the orthosteric site where acetylcholine binds. Many compounds which act as allosteric modulators of the α4β2 receptors have been identified, with both positive and negative effects. Such allosteric modulators either increase or decrease the response induced by agonist on the α4β2 receptors. Here we discuss the concept of allosterism as it pertains to the α4β2 receptors and summarize the important features of allosteric modulators for this nicotinic receptor subtype.
烟碱型乙酰胆碱受体是配体门控的离子通道，属于 Cys 环受体超家族。α4β2 亚基是脑内烟碱受体的主要异源二聚体亚基。α4β2 受体的变构调节剂与乙酰胆碱结合的正位结合位点不同，作用于其他位点。已经发现许多化合物可作为α4β2 受体的变构调节剂，具有正性和负性作用。这种变构调节剂可增加或减少激动剂诱导的α4β2 受体的反应。本文讨论了变构作用的概念及其与α4β2 受体的关系，并总结了该烟碱受体亚型的变构调节剂的重要特征。
