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Optically active benzamides as predictive tools for mapping the dopamine D2 receptor.

D Rognan1, P Sokoloff, A Mann

  • 1Centre de Neurochimie du CNRS, Département de Pharmacochimie Moléculaire, Strasbourg, France.

European Journal of Pharmacology
|July 31, 1990
PubMed
Summary

Structure-activity relationships of D2 dopamine antagonists were explored. A novel pharmacophore model, focusing on lone pair orientation, explains unusual stereoselectivity and guides new drug design.

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Area of Science:

  • Medicinal Chemistry
  • Neuropharmacology
  • Structural Biology

Background:

  • Sulpiride is a selective D2 dopamine antagonist.
  • Understanding structure-activity relationships (SAR) is crucial for drug development.
  • Stereochemistry significantly influences the activity of D2 antagonists.

Purpose of the Study:

  • To elucidate unusual SAR of N-substituted sulpiride analogs.
  • To develop a pharmacophore model for D2 dopamine antagonists.
  • To guide the design of novel D2 antagonist compounds.

Main Methods:

  • Pharmacophore modeling based on crystallographic data of (-)piquindone.
  • Extension of the model to include 14 other D2 antagonists.
  • Synthesis and in vitro/in vivo testing of designed compounds.

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Main Results:

  • A pharmacophore model emphasizing lone pair orientation was established.
  • Two distinct active conformations were identified for benzamides.
  • The model successfully predicted activities of synthesized compounds.

Conclusions:

  • The proposed pharmacophore model accurately explains stereoselective D2 antagonist activity.
  • The model provides a framework for designing novel D2 antagonists with specific properties.
  • This research advances the understanding of D2 receptor-ligand interactions.