Serotonin 5-HT<inf>7</inf> receptor antagonists

M. L. López-Rodríguez, B. Benhamú, M. J. Morcillo, E. Porras, J. L. Lavandera, L. Pardo

Research output: Contribution to journalReview articleResearchpeer-review

19 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)203-214
JournalCurrent Medicinal Chemistry - Central Nervous System Agents
Issue number3
Publication statusPublished - 1 Sep 2004


  • 5-HT receptor antagonists 7
  • Computational model
  • Ligand-receptor interaction
  • Pharmacophore model
  • Serotonin


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