Sigma-2 receptor

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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 suggested to be the putative 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[edit]

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

See also[edit]


  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. PMID 16845227. 
  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. doi:10.1016/j.ceca.2006.03.004. PMID 16687172. 
  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): 380. doi:10.1038/ncomms1386. PMID 21730960. 
  4. ^ Bowen WD (March 2000). "Sigma receptors: recent advances and new clinical potentials". Pharm Acta Helv 74 (2–3): 211–8. doi:10.1016/S0031-6865(99)00034-5. PMID 10812960. 
  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. doi:10.1016/j.bmcl.2010.03.009. PMID 20347592. 
  6. ^ Cassano, G; Gasparre, G; Niso, M; Contino, M; Scalera, V; Colabufo, NA (Apr 2009). "F281, synthetic agonist of the sigma-2 receptor, induces Ca2+ efflux from the endoplasmic reticulum and mitochondria in SK-N-SH cells.". Cell calcium 45 (4): 340–5. doi:10.1016/j.ceca.2008.12.005. PMID 19187959. 
  7. ^ a b Xu, J; Tu, Z; Jones, LA; Vangveravong, S; Wheeler, KT; Mach, RH (Nov 21, 2005). "[3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe.". European Journal of Pharmacology 525 (1-3): 8–17. doi:10.1016/j.ejphar.2005.09.063. PMID 16289030. 
  8. ^ 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. doi:10.1016/j.bmcl.2003.09.083. 
  9. ^ 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. doi:10.1016/j.ejphar.2005.09.063. PMID 16289030. 
  10. ^ Ghelardini, C; Galeotti, N; Bartolini, A (Nov 2000). "Pharmacological identification of SM-21, the novel sigma(2) antagonist.". Pharmacology, Biochemistry, and Behavior 67 (3): 659–62. doi:10.1016/s0091-3057(00)00405-6. PMID 11164098. 
  11. ^ 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. doi:10.1021/jm0614883. 
  12. ^ 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. doi:10.1021/jm970692a. 

External links[edit]