Serotonin 5-HT7 Receptor Antagonists

Title: Serotonin 5-HT7 Receptor Antagonists

Volume: 4 Issue: 3

Author(s): M. L. Lopez-Rodriguez, B. Benhamu, M. J. Morcillo, E. Porras, J. L. Lavandera and L. Pardo

Affiliation:

Keywords: serotonin, 5-ht7 receptor antagonists, pharmacophore model, computational model, ligand-receptor interaction

Abstract: The 5-HT7R is the most recent addition to the burgeoning family of serotonin receptors. Preliminary evidences suggest that it may be involved in depression, control of circadian rhythms, and relaxation in a variety of vascular smooth muscles, indicating the high potential of 5-HT7R ligands as new therapeutic drugs. During the last four years several selective 5-HT7R antagonists have been discovered, and we have recently contributed to this field with the definition of a pharmacophoric hypothesis for 5-HT7R antagonism and a computational model of ligand-receptor interaction of new naphtholactam and naphthosultam derivatives acting at this receptor. This article will review the development of 5-HT7R antagonists with an emphasis on selective antagonists, their structural requirements and ligand-receptor interactions, as well as the potential therapeutic opportunities surrounding 5-HT7R ligands.

Cite this article as:

Lopez-Rodriguez L. M., Benhamu B., Morcillo J. M., Porras E., Lavandera L. J. and Pardo L., Serotonin 5-HT7 Receptor Antagonists, Current Medicinal Chemistry - Central Nervous System Agents 2004; 4 (3) . https://dx.doi.org/10.2174/1568015043356931