PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

We synthesized [F-18]FCWAY, an analog of [carbonyl-C-11]WAY-100635 ([C-11]N-(2-(1-(4(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridinyl))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 [F-18]FC and [F-18]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 [F-18]FCWAY has very similar kinetic characteristics to [C-11]WAY-100635. NUCL MED BIOL 27;5:493-497, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.