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The sigma-2 receptor (σ2R) is a sigma receptor subtype which preferentially binds to siramesine[1] and PB28.[2] PGRMC1 was recently identified as the sigma-2 receptor.[3] Unlike sigma-1 receptor, it has not yet been cloned.

Activation of the receptor can cause apoptosis.[4] A pharmacophore model based on benzooxazolone derivatives has been developed.[5]

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[6][7]
  • 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[8]
  • 3,3-Dimethyl-1-[5-(1,2,3,4-tetrahydronaphthalen-1-yl)-n-pentyl]piperidine[9]

See also[]


  1. Skuza G, Rogóz Z (2006). The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J. Physiol. Pharmacol. 57 (2): 217–29.
  2. Cassano G, Gasparre G, Contino M, et al (2006). The sigma-2 receptor agonist PB28 inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells. Cell Calcium 40 (1): 23–8.
  3. Xu J, Zeng C, Chu W, et al (2011). Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site. Nature Communications 380 (2).
  4. Bowen WD (March 2000). Sigma receptors: recent advances and new clinical potentials. Pharm Acta Helv 74 (2–3): 211–8.
  5. Laurini E, Zampieri D, Mamolo MG, Vio L, Zanette C, Florio C, Posocco P, Fermeglia M, Pricl S (May 2010). A 3D-pharmacophore model for sigma2 receptors based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives. Bioorg. Med. Chem. Lett. 20 (9): 2954–7.
  6. Mach RH, Huang Y, Freeman RA, Wu L, Vangveravong S, Luedtke RR (2004). Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands. Bioorg. Med. Chem. Lett. 14 (1): 195–202.
  7. Xu J, Tu Z, Jones LA, Vangveravong S, Wheeler KT, Mach RH (2005). [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methyl benzamide: a novel sigma-2 receptor probe. Eur. J. Pharmacol. 525 (1-3): 8–17.
  8. Tu Z, Xu J, Jones LA, Li S, Dumstorff C, Vangveravong S, Chen DL, Wheeler KT, Welch MJ, Mach RH (2007). Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography. J. Med. Chem. 50 (14): 3194–204.
  9. Berardi F, Santoro S, Perrone R, Tortorella V, Govoni S, Lucchi L (1998). N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands. J. Med. Chem. 41 (21): 3940–7.

External links[]


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