Sigma-2 receptor

The sigma-2 receptor (σ2R) is a sigma receptor which preferentially binds to siramesine and PB28. Unlike sigma-1 receptor, it has not yet been cloned.

Activation of the receptor can cause apoptosis. A pharmacophore model based on benzooxazolone derivatives.

Sigma-2 ligand binding in vitro
Tumor cells were incubated with 10 nM of SW120 (a fluorescent-labeled sigma-2 receptor ligand) for 30 minutes. HPDE cells were used as a normal control. To demonstrate the specificity of SW120 for Sigma-2 receptor binding, 10μM of SV95 (Sigma-2 ligand) or (+)-pentazocine (sigma-1 receptor ligand) were added to cells 30 minutes prior to SW120 treatment. All lines were then washed 3 times with PBS and evaluated by flow cytometry.