Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2)

Bioorg Med Chem. 2010 Feb;18(3):1204-12. doi: 10.1016/j.bmc.2009.12.039. Epub 2009 Dec 21.

Abstract

In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards sigma(1)- and sigma(2)-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry
  • Alkenes / pharmacology
  • Amines / chemistry*
  • Amines / pharmacology*
  • Amino Alcohols / chemistry
  • Amino Alcohols / pharmacology
  • Animals
  • Guinea Pigs
  • Hydrocarbons, Aromatic / chemistry
  • Hydrocarbons, Aromatic / pharmacology
  • Ligands
  • Models, Molecular
  • Protein Binding
  • Rats
  • Receptors, Opioid / metabolism
  • Receptors, sigma / metabolism*
  • Structure-Activity Relationship

Substances

  • Alkenes
  • Amines
  • Amino Alcohols
  • Hydrocarbons, Aromatic
  • Ligands
  • Receptors, Opioid
  • Receptors, sigma