5-HT7 Receptor Antagonists with an Unprecedented Selectivity Profile

ChemMedChem. 2018 Apr 23;13(8):795-802. doi: 10.1002/cmdc.201800026. Epub 2018 Mar 30.

Abstract

Selective leads: In this study, we generated a new series of serotonin 5-HT7 receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT7 antagonists with unprecedented high selectivity for the 5-HT7 receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.

Keywords: 5-HT7 receptor; antagonists; selectivity; serotonin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • HEK293 Cells
  • Humans
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / chemistry*
  • Serotonin Antagonists / pharmacology*
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship

Substances

  • Isoquinolines
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Small Molecule Libraries
  • serotonin 7 receptor