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

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.