PET evaluation of [(18)F]FCWAY, an analog of the 5-HT(1A) receptor antagonist, WAY-100635

Nucl Med Biol. 2000 Jul;27(5):493-7. doi: 10.1016/s0969-8051(00)00118-9.


We synthesized [(18)F]FCWAY, an analog of [carbonyl-(11)C]WAY-100635 ¿[(11)C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridi nyl))cyclohexanecarboxamide¿, by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [(18)F]FC and [(18)F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [(18)F]FCWAY has very similar kinetic characteristics to [(11)C]WAY-100635.

MeSH terms

  • Animals
  • Fluorine Radioisotopes*
  • Humans
  • Macaca mulatta
  • Models, Biological
  • Piperazines / metabolism*
  • Pyridines / metabolism*
  • Receptors, Serotonin / analysis*
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists / metabolism*
  • Tomography, Emission-Computed*


  • Fluorine Radioisotopes
  • Piperazines
  • Pyridines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide