Sigma-2 receptor

The sigma-2 receptor (σ2R) is a sigma receptor subtype which preferentially binds to siramesine and PB28. PGRMC1 was recently identified as the sigma-2 receptor. Unlike sigma-1 receptor, it has not yet been cloned.

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

Selective ligands
Several ligands with high affinity and selectivity for the σ2 receptor over the σ1 receptor have been reported:


 * BIMU-1
 * CB-184
 * PB28
 * RHM-2
 * siramesine
 * WC-59
 * (N-[4-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-butyl]-2-(2-fluoro-ethoxy)-3-methoxy-5-iodo-benzamide
 * 3,3-Dimethyl-1-[5-(1,2,3,4-tetrahydronaphthalen-1-yl)-n-pentyl]piperidine