In search of potent 5-HT6 receptor inverse agonists

Chem Biol Drug Des. 2014 Jun;83(6):666-9. doi: 10.1111/cbdd.12279.

Abstract

A series of non-sulfonamide/non-sulfone derived potent 5-HT6 receptor inverse agonists has been disclosed. Representative compound 9 (Ki = 14 nm) displayed selectivity against a set of family members as well as brain permeability 6 h post-oral administration. In addition, the separated enantiomers of compound 9 displayed difference in activity indicating the influence of chirality on potency.

Keywords: 5-HT6 receptor; CNS disorders; benzazepine.

Publication types

  • Letter

MeSH terms

  • Benzazepines / chemistry
  • Benzazepines / pharmacology
  • Biological Assay
  • Drug Inverse Agonism*
  • Humans
  • Molecular Structure
  • Protein Binding / drug effects
  • Receptors, Serotonin / chemistry*
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology
  • Sulfones / chemistry
  • Sulfones / pharmacology

Substances

  • Benzazepines
  • Receptors, Serotonin
  • Sulfonamides
  • Sulfones
  • serotonin 6 receptor