Chukchi Campus, Department of Bio-science, College of Rural and Community Development, University of Alaska Fairbanks, P.O. Box 297, Kotzebue, AK 99752-0297, USA.
Biochem Pharmacol. 2013 Oct 15;86(8):1054-62. doi: 10.1016/j.bcp.2013.05.018. Epub 2013 May 31.
Nicotinic acetylcholine receptors (nAChRs) are ligand-gated cation-conducting transmembrane channels from the cys-loop receptor superfamily. The neuronal subtypes of these receptors (e.g. the α7 and α4β2 subtypes) are involved in neurobehavioral processes such as anxiety, the central processing of pain, food intake, nicotine seeking behavior, and a number of cognitive functions like learning and memory. Neuronal nAChR dysfunction is involved in the pathophysiology of many neurological disorders, and behavioral studies in animals are useful models to assess the effects of compounds that act on these receptors. Allosteric modulators are ligands that bind to the receptors at sites other than the orthosteric site where acetylcholine, the endogenous agonist for the nAChRs, binds. While conventional ligands for the neuronal nAChRs have been studied for their behavioral effects in animals, allosteric modulators for these receptors have only recently gained attention, and research on their behavioral effects is growing rapidly. Here we will discuss the behavioral effects of allosteric modulators of the neuronal nAChRs.
烟碱型乙酰胆碱受体（nAChRs）是配体门控阳离子通道，属于细胞外环受体超家族。这些受体的神经元亚型（例如α7 和 α4β2 亚型）参与神经行为过程，如焦虑、疼痛的中枢处理、食物摄入、尼古丁寻求行为以及许多认知功能，如学习和记忆。神经元 nAChR 功能障碍与许多神经疾病的病理生理学有关，动物的行为研究是评估作用于这些受体的化合物影响的有用模型。变构调节剂是与乙酰胆碱（nAChRs 的内源性激动剂）结合的正位点以外的受体结合的配体。虽然已经研究了传统的神经元 nAChR 配体对动物的行为影响，但这些受体的变构调节剂最近才受到关注，并且对其行为影响的研究正在迅速发展。在这里，我们将讨论神经元 nAChR 的变构调节剂的行为影响。
