D1 agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: A structure-activity study

Sergio Mantegani, Emanuele Arlandini, Tiziano Bandiera, Daniela Borghi, Enzo Brambilla, Carla Caccia, Maria Antonietta Cervini, Paolo Cremonesi, Robert Albert McArthur, Gabriella Traquandi, Mario Varasi

Research output: Contribution to journalArticle

Abstract

A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure- activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.

Original languageEnglish
Pages (from-to)107-124
Number of pages18
JournalEuropean Journal of Medicinal Chemistry
Volume34
Issue number2
DOIs
Publication statusPublished - Feb 1999

    Fingerprint

Keywords

  • Antidopaminergic activity
  • Dopaminergic
  • Ergoline derivatives
  • Structure-affinity relationship

ASJC Scopus subject areas

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

Cite this

Mantegani, S., Arlandini, E., Bandiera, T., Borghi, D., Brambilla, E., Caccia, C., Cervini, M. A., Cremonesi, P., McArthur, R. A., Traquandi, G., & Varasi, M. (1999). D1 agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: A structure-activity study. European Journal of Medicinal Chemistry, 34(2), 107-124. https://doi.org/10.1016/S0223-5234(99)80045-2