Sigma 1 receptor agonist/antagonist

Sigma-1 receptor (Sig-1R) is an endoplasmic reticulum protein (ER) localized in the the mitochondria-associated endoplasmic reticulum membrane (MAM), an ER –mitochondria interface.

Sig-1R is a multipotent regulator, by interacting with many proteins from different classes (Su et al., Trends in Pharmacological Science, in press).

We developed an original fast-screening in vitro assay based from the observation that the Sig-1R chaperone association to BiP is specifically modulated by agonistic activity of ligands (Meunier & Hayashi, J Pharmacol Exp Ther,2009, Fujimoti et al., Synapse, 2012). By using high affinity ELISA assay, this activity test allows a fast determination of agonist or antagonist property of tested compound.