Serotonin 5-HT7 Receptor Antagonists

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

Journal Name: Current Medicinal Chemistry - Central Nervous System Agents
Continued as Central Nervous System Agents in Medicinal Chemistry

Volume 4 , Issue 3 , 2004


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

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Article Details

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

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