Current Medicinal Chemistry - Central Nervous System Agents

Back

Serotonin 5-HT7 Receptor Antagonists

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

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.

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

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 4
ISSUE: 3
Year: 2004
Page: [203 - 214]
Pages: 12
DOI: 10.2174/1568015043356931
Price: $58