5(10→9)abeo-ergoline derivatives: Synthesis, 5-HT(1A)-receptor affinity and selectivity

Sergio Mantegani, Luca Baumer, Enzo Brambilla, Carla Caccia, Maria Gioia Fornaretto, Robert Albert McArthur, Mario Varasi

Research output: Contribution to journalArticlepeer-review

Abstract

The synthesis and the structure-affinity relationship (S.A.F.I.R.) study for the 5-HT(1A) receptor sites of a novel series of 5(10→9)abeo-ergoline derivatives are presented. Most derivatives showed moderate to high affinity and selectivity for 5-HT(1A) receptor sites. The structure-affinity relationship pointed out the role of the substituent at position 8, and the outstanding importance of the reduction of the indole 2,3-double bond for achieving the highest 5-HT(1A) affinity and selectivity within the compounds presented.

Original languageEnglish
Pages (from-to)279-292
Number of pages14
JournalEuropean Journal of Medicinal Chemistry
Volume33
Issue number4
DOIs
Publication statusPublished - Apr 1998

Keywords

  • 5(10→9)abeo-ergoline derivative
  • 5-HT(1A) receptor ligand
  • Ergoline derivative
  • Serotonin
  • Structure-affinity relationship

ASJC Scopus subject areas

  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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