Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8. doi: 10.1016/j.bmcl.2005.06.024.

Abstract

High-throughput screening of an array of biphenylmethylamines synthesised by high-throughput solid-phase chemistry resulted in the identification of compounds with high-affinity for the 5-ht5A receptor. The structure-activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11, a potent and selective 5-ht5A receptor antagonist.

MeSH terms

  • Animals
  • Cell Line
  • Cricetinae
  • Drug Evaluation, Preclinical*
  • Guanosine 5'-O-(3-Thiotriphosphate) / pharmacology
  • Guinea Pigs
  • Humans
  • Molecular Structure
  • Radioligand Assay
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / chemical synthesis
  • Serotonin Antagonists / chemistry*
  • Serotonin Antagonists / metabolism
  • Serotonin Antagonists / pharmacology*
  • Structure-Activity Relationship

Substances

  • Receptors, Serotonin
  • Serotonin Antagonists
  • serotonin 5 receptor
  • Guanosine 5'-O-(3-Thiotriphosphate)