Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach

Mini Rev Med Chem. 2005 Oct;5(10):927-40. doi: 10.2174/138955705774329519.

Abstract

At least two different types of sigma (sigma1 and sigma2) receptors have been identified. A structural feature common to high-affinity (Ki <10 nM) sigma1 ligands is: C-N(R)-X-Ph; both C and Ph are associated with regions of bulk tolerance. Numerous other ligands bind, but typically do so with lower affinity.

Publication types

  • Review

MeSH terms

  • Amines / chemical synthesis
  • Amines / pharmacology*
  • Animals
  • Humans
  • Ligands
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology*
  • Piperidines / chemical synthesis
  • Piperidines / pharmacology*
  • Protein Binding
  • Receptors, Drug / metabolism*
  • Receptors, sigma / metabolism*

Substances

  • Amines
  • Ligands
  • Piperazines
  • Piperidines
  • Receptors, Drug
  • Receptors, sigma