Synthesis of novel analogs of cabergoline: Improving cardiovascular safety by removing 5-HT2B receptor agonism

Peter I. Dosa, Tim Ward, Michael A. Walters, Suck Won Kim

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

The dopamine agonist cabergoline has been used to treat prolactinomas, Parkinson's disease, Cushing's disease, and sexual dysfunction. However, its clinical use was severely curtailed when it was found that patients taking cabergoline had an increased risk of developing cardiac-valve regurgitation. This potentially life-threatening condition has been associated with drugs, such as cabergoline, that are 5-HT2B receptor agonists. We prepared analogs of cabergoline and have identified several that have limited or no agonism at the 5-HT2B receptor.

Original languageEnglish (US)
Pages (from-to)254-258
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume4
Issue number2
DOIs
StatePublished - Feb 14 2013

Keywords

  • 5-HT2B
  • Cabergoline
  • dopamine agonist
  • ergot alkaloid
  • sexual dysfunction

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