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Amisulpride, Sultopride and Sulpiride: Comparison of Conformational and Physico-Chemical Properties

  • Audrey Blomme
  • Laurence Conraux
  • Philippe Poirier
  • Anne Olivier
  • Jean-Jacques Koenig
  • Mireille Sevrin
  • François Durant
  • Pascal George

Abstract

Amisulpride, sultopride and sulpiride (Figure 1) are antagonists of the D2-like dopamine receptors, which are members of a large family of receptors that interact with specific intracellular signalling pathways through coupling with G proteins. These compounds are substituted benzamides and present a high degree of selectivity for D2 and D3 versus D1 and D4 dopaminergic receptor subtypes. Amisulpride, sultopride and sulpiride respectively present decreasing in vitro affinities for the D2 receptor (IC50 = 27, 120 and 181 nM) and the D3 receptor (IC50 = 3.6, 4.8 and 17.5 nM).

Keywords

High Occupy Molecular Orbital Lower Unoccupied Molecular Orbital High Occupy Molecular Orbital Lower Unoccupied Molecular Orbital Conformational Space 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Copyright information

© Springer Science+Business Media New York 2000

Authors and Affiliations

  • Audrey Blomme
    • 1
  • Laurence Conraux
    • 2
  • Philippe Poirier
    • 2
  • Anne Olivier
    • 3
  • Jean-Jacques Koenig
    • 2
  • Mireille Sevrin
    • 3
  • François Durant
    • 1
  • Pascal George
    • 3
  1. 1.Laboratoire de Chimie Moléculaire StructuraleFacultés UniversitairesNamurBelgium
  2. 2.Groupe de Biochimie Moléculaire StructuraleSynthélabo RechercheRueilFrance
  3. 3.Département de Recherche SNCSynthélabo RechercheBagneuxFrance

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