@MISC{_invivo, author = {}, title = {In Vivo Kinetics of [F-18]MEFWAY: A Comparison With [C-11]WAY100635 and [F-18]MPPF in the Nonhuman Primate}, year = {} }
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Abstract
ABSTRACT [F-18]Mefway was developed to provide an F-18 labeled positron emis-sion tomography (PET) neuroligand with high affinity for the serotonin 5-HT1A receptor to improve the in vivo assessment of the 5-HT1A system. The goal of this work was to compare the in vivo kinetics of [F-18]mefway, [F-18]MPPF, and [C-11]WAY100635 in the rhesus monkey. Methods: Each of four monkeys were given bolus injections of [F-18]mefway, [C-11]WAY100635, and [F-18]MPPF and scans were acquired with a micro-PET P4 scanner. Arterial blood was sampled to assay parent compound throughout the time course of the PET experiment. Time activity curves were extracted in the high 5-HT1A binding areas of the anterior cingulate cortex (ACG), mesial temporal cortex, raphe nuclei, and insula cortex. Time activity curves were also extracted in the cerebel-lum, which was used as a reference region. The in vivo kinetics of the radiotracers were compared based on the nondisplaceable distribution volume (VND) and binding potential (BPND). Results: At 30 min, the fraction of radioactivity in the plasma due to parent compound was 19%, 28%, and 29 % and cleared from the arterial plasma at rates of 0.0031, 0.0078, and 0.0069 (min21) ([F-18]mefway, [F-18]MPPF, [C-11]WAY100635). The BPND in the brain regions were mesial temporal cortex: 7.4 6 0.6, 3.1 6 0.4, 7.0 6 1.2,