Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II

Bioorg Med Chem. 2009 Jan 15;17(2):758-66. doi: 10.1016/j.bmc.2008.11.044. Epub 2008 Nov 24.

Abstract

In the search for compounds with potential for development as positron emission tomography radioligands for brain D(3) receptor imaging, a series of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides with appropriate lipophilicity (2<logP<3.5) were synthesized and tested in vitro. Some of the final compounds showed moderate-to-high dopamine D(3) receptor affinities but lacked selectivity over D(2) receptors.

MeSH terms

  • Amides / chemical synthesis*
  • Drug Design
  • Humans
  • Ligands
  • Piperazines / chemical synthesis*
  • Positron-Emission Tomography / methods*
  • Protein Binding
  • Radiopharmaceuticals
  • Receptors, Dopamine D3 / analysis*
  • Receptors, Dopamine D3 / metabolism

Substances

  • Amides
  • Ligands
  • Piperazines
  • Radiopharmaceuticals
  • Receptors, Dopamine D3