Sign in
Back
Thioxanthene-derived analogs as sigma(1) receptor ligands
Journal article   Peer reviewed

Thioxanthene-derived analogs as sigma(1) receptor ligands

Richard A Glennon, Abd M Ismaiel, Seth Ablordeppey, Mahmoud El-Ashmawy, James B Fisher and Abdulkhader M. Ismaiel
Bioorganic & medicinal chemistry letters, Vol.14(9), pp.2217-2220
03/05/2004
DOI: https://doi.org/10.1016/j.bmcl.2004.02.018
PMID: 15081012

Abstract

Ligands Receptors, sigma - metabolism Structure-Activity Relationship Thioxanthenes - chemistry Thioxanthenes - metabolism
An investigation of the structure-affinity relationships for the binding of thioxanthene-related structures indicates that an intact thioxanthene ring is not required for binding at sigma(1) receptors, and that with the appropriate structural modifications, affinity can be enhanced to the subnanomolar level. Certain of the analogs displayed sigma(1)-fold selectivity for sigma(1) versus sigma(2) receptors.

Metrics

1 Record Views

Details