Synthesis and in vitro structure-activity relationship of 13-tert- butyl-ergoline derivatives as 5-HT(1A) receptor ligands

S. Mantegani, E. Brambilla, C. Caccia, M. G. Fornaretto, R. A. Mc Arthur, M. Varasi

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT(1A) receptors versus α1, α2, D1, D2, and 5- HT2 appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT(1A) affinity and hundred-fold selectivity versus the other receptors considered.

Original languageEnglish
Pages (from-to)795-804
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume32
Issue number10
DOIs
Publication statusPublished - Oct 1997

Fingerprint

Ergolines
Receptor, Serotonin, 5-HT1A
Structure-Activity Relationship
Ligands
Derivatives
Skeleton
Adrenergic Agents
Serotonin
In Vitro Techniques

Keywords

  • 13-tert-butyl-ergoline
  • 5-HT(1A) affinity
  • Ergoline derivative
  • Selectivity

ASJC Scopus subject areas

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

Cite this

Synthesis and in vitro structure-activity relationship of 13-tert- butyl-ergoline derivatives as 5-HT(1A) receptor ligands. / Mantegani, S.; Brambilla, E.; Caccia, C.; Fornaretto, M. G.; Mc Arthur, R. A.; Varasi, M.

In: European Journal of Medicinal Chemistry, Vol. 32, No. 10, 10.1997, p. 795-804.

Research output: Contribution to journalArticle

Mantegani, S. ; Brambilla, E. ; Caccia, C. ; Fornaretto, M. G. ; Mc Arthur, R. A. ; Varasi, M. / Synthesis and in vitro structure-activity relationship of 13-tert- butyl-ergoline derivatives as 5-HT(1A) receptor ligands. In: European Journal of Medicinal Chemistry. 1997 ; Vol. 32, No. 10. pp. 795-804.
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