Sigma-2 receptor

From Wikipedia, the free encyclopedia

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

References

  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). 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. ↑ 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. doi:10.1016/j.ejphar.2005.09.063. 
  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. doi:10.1021/jm0614883. 
  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. doi:10.1021/jm970692a. 

External links


G protein-coupled receptor
Hormone receptors
Hypothalamic
Pituitary
Other
Opioid receptors
Other neuropeptide receptors
Type I cytokine receptor
Enzyme-linked receptor
Other
B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
Receptor
Ligands
Unknown


This article is issued from Wikipedia. The text is available under the Creative Commons Attribution/Share Alike; additional terms may apply for the media files.