Sigma-2 receptor

Sigma-2 receptor

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

External links

  • Medical Subject Headings (MeSH)