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. 2012 Apr;22(4):308-17.
doi: 10.1016/j.euroneuro.2011.08.002. Epub 2011 Sep 10.

Evaluation of sigma (σ) receptors in the antidepressant-like effects of ketamine in vitro and in vivo

Matthew J Robson  1 , Meenal Elliott, Michael J Seminerio, Rae R Matsumoto
Affiliations

Evaluation of sigma (σ) receptors in the antidepressant-like effects of ketamine in vitro and in vivo

Matthew J Robson et al. Eur Neuropsychopharmacol. 2012 Apr.

Abstract

Ketamine is an NMDA antagonist and dissociative anesthetic that has been shown to display rapid acting and prolonged antidepressant activity in small-scale human clinical trials. Ketamine also binds to σ receptors, which are believed to be protein targets for a potential new class of antidepressant medications. The purpose of this study was to determine the involvement of σ receptors in the antidepressant-like actions of ketamine. Competition binding assays were performed to assess the affinity of ketamine for σ(1) and σ(2) receptors. The antidepressant-like effects of ketamine were assessed in vitro using a neurite outgrowth model and PC12 cells, and in vivo using the forced swim test. The σ receptor antagonists, NE-100 and BD1047, were evaluated in conjunction with ketamine in these assays to determine the involvement of σ receptors in the antidepressant-like effects of ketamine. Ketamine bound to both σ(1) and σ(2) receptors with μM affinities. Additionally, ketamine potentiated NGF-induced neurite outgrowth in PC12 cells and this effect was attenuated in the presence of NE-100. Ketamine also displayed antidepressant-like effects in the forced swim test; however, these effects were not attenuated by pretreatment with NE-100 or BD1047. Taken together, these data suggest that σ receptor-mediated neuronal remodeling may contribute to the antidepressant effects of ketamine.

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