PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635
pmid: 10962257
PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635
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.
- National Institute of Health Pakistan
- National Institutes of Health United States
Fluorine Radioisotopes, Pyridines, Macaca mulatta, Models, Biological, Piperazines, Receptors, Serotonin, Animals, Humans, Serotonin Antagonists, Receptors, Serotonin, 5-HT1, Tomography, Emission-Computed
Fluorine Radioisotopes, Pyridines, Macaca mulatta, Models, Biological, Piperazines, Receptors, Serotonin, Animals, Humans, Serotonin Antagonists, Receptors, Serotonin, 5-HT1, Tomography, Emission-Computed
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