Allosteric Modulation of Sigma-1 Receptors Elicits Rapid Antidepressant Activity.

ABSTRACT:

Aims

Sigma-1 receptors are involved in the pathophysiological process of several neuropsychiatric diseases such as epilepsy, depression. Allosteric modulation represents an important mechanism for receptor functional regulation. In this study, we examined antidepressant activity of the latest identified novel and selective allosteric modulator of sigma-1 receptor 3-methyl-phenyl-2, 3, 4, 5-tetrahydro-1H-benzo[d]azepin-7-ol (SOMCL-668).

Methods and results

A single administration of SOMCL-668 decreased the immobility time in the forced swimming test (FST) and tailing suspended test in mice, which were abolished by pretreatment of sigma-1 receptor antagonist BD1047. In the chronic unpredicted mild stress (CUMS) model, chronic application of SOMCL-668 rapidly ameliorated anhedo

SUBMITTER: Wang Y 

PROVIDER: S-EPMC6492821 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature