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|Title:||In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [C-11]befloxatone and the multi-injection approach.|
Positron computed tomography
|Publisher:||Nature Publishing Group|
|Citation:||Bottlaender, M., Valette, H., Delforge, J., Saba, W., Guenther, I., Curet, O., George, P., Dollé, F., & Gregoire, M. C. (2010). In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [C-11]befloxatone and the multi-injection approach. Journal of Cerebral Blood Flow and Metabolism, 30(4), 792-800. doi:10.1038/jcbfm.2009.242|
|Abstract:||[C-11]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 [C-11] 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 (KdVR = 6.4 +/- 1.5 nmol/L). This study is the first PET-based estimation of the B-max of an enzyme. © 2010, Nature Publishing Group.|
|Gov't Doc #:||5690|
|Appears in Collections:||Journal Articles|
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