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- W2084094587 abstract "[ 11 C]befloxatone is a high-affinity, reversible, and selective radioligand for the in vivo visualization of the monoamine oxidase A (MAO-A) binding sites using positron emission tomography (PET). The multi-injection approach was used to study in baboons the interactions between the MAO-A binding sites and [ 11 C]befloxatone. The model included four compartments and seven parameters. The arterial plasma concentration, corrected for metabolites, was used as input function. The experimental protocol—three injections of labeled and/or unlabeled befloxatone—allowed the evaluation of all the model parameters from a single PET experiment. In particular, the brain regional concentrations of the MAO-A binding sites ( B′ max ) and the apparent in vivo befloxatone affinity ( K d ) were estimated in vivo for the first time. A high binding site density was found in almost all the brain structures (170±39 and 194±26 pmol/mL in the frontal cortex and striata, respectively, n=5). The cerebellum presented the lowest binding site density (66±13 pmol/mL). Apparent affinity was found to be similar in all structures ( K d V R =6.4±1.5 nmol/L). This study is the first PET-based estimation of the B max of an enzyme." @default.
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- W2084094587 date "2009-11-18" @default.
- W2084094587 modified "2023-10-15" @default.
- W2084094587 title "<i>In vivo</i> Quantification of Monoamine Oxidase A in Baboon Brain: A PET Study Using [<sup>11</sup>C]befloxatone and the Multi-Injection Approach" @default.
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- W2084094587 doi "https://doi.org/10.1038/jcbfm.2009.242" @default.
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