Design and Radiofluorination of Benzamide Dopamine D2 Receptor Ligands

  • Tomas de Paulis
  • Danny R. Bingham
  • Ronald G. Manning
  • N. Scott Mason
  • M. Sib Ansari
  • Dennis E. Schmidt
  • Robert M. Kessler

Abstract

Remoxipride (Figure 1), a substituted benzamide analog of sulpiride, was developed as a potential antipsychotic agent on the assumption that the poor bioavailability of sulpiride was due to hydrolysis of the amide bond.1 In the rat, remoxipride was shown to be 10 times weaker than sulpiride in blocking dopamine D2 receptors in vitro, but in vivo was 50 times more potent.2 This observation led to the development of the 6-methoxysalicylamide series, of which raclopride is the best known member and eticlopride is the most potent.3

Keywords

Radiochemical Yield Tosyl Chloride Spiperone Binding Eighth International Symposium Allyl Phenol 
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Copyright information

© Springer Science+Business Media New York 1991

Authors and Affiliations

  • Tomas de Paulis
    • 1
  • Danny R. Bingham
    • 1
  • Ronald G. Manning
    • 1
  • N. Scott Mason
    • 1
  • M. Sib Ansari
    • 1
  • Dennis E. Schmidt
    • 2
  • Robert M. Kessler
    • 1
    • 2
  1. 1.Departments of RadiologyVanderbilt University School of MedicineNashvilleUSA
  2. 2.Departments of PsychiatryVanderbilt University School of MedicineNashvilleUSA

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