Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors

Li Fang Yu, Han Kun Zhang, Barbara J. Caldarone, J. Brek Eaton, Ronald J. Lukas, Alan P. Kozikowski

Research output: Contribution to journalArticlepeer-review

30 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)8204-8223
Number of pages20
JournalJournal of medicinal chemistry
Issue number20
StatePublished - Oct 23 2014

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


Dive into the research topics of 'Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors'. Together they form a unique fingerprint.

Cite this