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Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.

Abstract：

: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 α4β2-nAChRs in depression, along with the structural features that are essential to ligand recognition by the α4β2-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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Yu LF,Zhang HK,Caldarone BJ,Eaton JB,Lukas RJ,Kozikowski AP

doi

10.1021/jm401937a

subject

Has Abstract

pub_date

2014-10-23 00:00:00

pages

8204-23

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章,评审

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