Recent Developments in Novel Antidepressants Targeting 伪4尾2-Nicotinic Acetylcholine Receptors

详细信息    查看全文

• 作者：Li-Fang Yu ; Han-Kun Zhang ; Barbara J. Caldarone ; J. Brek Eaton ; Ronald J. Lukas ; Alan P. Kozikowski
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：October 23, 2014
• 年：2014
• 卷：57
• 期：20
• 页码：8204-8223
• 全文大小：903K
• ISSN：1520-4804

文摘

Nicotinic acetylcholine receptors (nAChRs) have been investigated for developing drugs that can potentially treat various central nervous system disorders. Considerable evidence supports the hypothesis that modulation of the cholinergic system through activation and/or desensitization/inactivation of nAChR holds promise for the development of new antidepressants. The introductory portion of this Miniperspective discusses the basic pharmacology that underpins the involvement of 伪4尾2-nAChRs in depression, along with the structural features that are essential to ligand recognition by the 伪4尾2-nAChRs. The remainder of this Miniperspective analyzes reported nicotinic ligands in terms of drug design considerations and their potency and selectivity, with a particular focus on compounds exhibiting antidepressant-like effects in preclinical or clinical studies. This Miniperspective aims to provide an in-depth analysis of the potential for using nicotinic ligands in the treatment of depression, which may hold some promise in addressing an unmet clinical need by providing relief from depressive symptoms in refractory patients.