[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7.

Abstract

Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET radioligand. Compound [(18)F]10 was prepared with high radiochemical purity and showed promising binding properties in rat brain imaging experiments.

MeSH terms

  • Aniline Compounds / chemistry*
  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism
  • Fluorine Radioisotopes* / blood
  • Imaging, Three-Dimensional
  • Molecular Structure
  • Positron-Emission Tomography*
  • Pyrazines / chemistry*
  • Pyrazoles / chemistry*
  • Pyrazoles / metabolism
  • Rats
  • Tissue Distribution

Substances

  • (18F)(R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one
  • Aniline Compounds
  • Fluorine Radioisotopes
  • Pyrazines
  • Pyrazoles