High-affinity fluorescent ligands for the 5-HT(3) receptor

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1151-5. doi: 10.1016/j.bmcl.2011.11.097. Epub 2011 Dec 1.

Abstract

The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT(3) receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT(3)AR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • COS Cells
  • Chlorocebus aethiops
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacology*
  • Humans
  • Ligands
  • Models, Molecular
  • Molecular Structure
  • Receptors, Serotonin, 5-HT3 / chemistry*
  • Receptors, Serotonin, 5-HT3 / metabolism
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Fluorescent Dyes
  • Ligands
  • Receptors, Serotonin, 5-HT3
  • Small Molecule Libraries