The current agonists and positive allosteric modulators of α 7 nAChR for CNS indications in clinical trials

Abstract The alpha-7 nicotinic acetylcholine receptor ( α 7 nAChR), consisting of homomeric α 7 subunits, is a ligand-gated Ca 2+ -permeable ion channel implicated in cognition and neuropsychiatric disorders. Enhancement of α 7 nAChR function is considered to be a potential therapeutic strategy aiming at ameliorating cognitive deficits of neuropsychiatric disorders such as Alzheimer's disease (AD) and schizophrenia. Currently, a number of α 7 nAChR modulators have been reported and several of them have advanced into clinical trials. In this brief review, we outline recent progress made in understanding the role of the α 7 nAChR in multiple neuropsychiatric disorders and the pharmacological effects of α 7 nAChR modulators used in clinical trials.