Structure-activity relationships of serotonin 5-HT7 receptors ligands: A review

Eur J Med Chem. 2019 Dec 1:183:111705. doi: 10.1016/j.ejmech.2019.111705. Epub 2019 Sep 16.

Abstract

5-HT7 receptors are the most recently discovered serotonergic receptors, for which numerous physiological implications in the central and the peripheral nervous systems as well as the endocrine system are described. A current public health challenge is to propose new and more efficient treatments against neuropsychiatric disorders such as epilepsy or Alzheimer's disease. In this context, 5-HT7 receptors represent an interesting target for the treatment and prevention of those pathologies, as an alternative or in association with other medicines. Thus, numerous chemical series of agonists and antagonists have been developed. Some of these molecules have shown a therapeutic potential in various in vivo studies. This review aims to present an overview of 5-HT7 receptors and of the medicinal chemistry programs that led to the identification of new, potent and selective 5-HT7 receptors ligands. Structure-activity relationships studies based on molecular docking and pharmacophoric approaches are also described.

Keywords: 5-HT(7) receptors; Medicinal chemistry; Molecular docking; Pharmacophore; Structure-activity relationships.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Ligands
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / chemistry
  • Serotonin Antagonists / pharmacology*
  • Serotonin Receptor Agonists / chemistry
  • Serotonin Receptor Agonists / pharmacology*
  • Structure-Activity Relationship

Substances

  • Ligands
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • serotonin 7 receptor