Abstract
In this chapter an example will be given of how the interaction of a newly developed pharmaceutical with a known PET radiotracer as a probe can be used on the one hand to improve tracer uptake measurement and on the other hand may contribute to the understanding of the action of the drug in peripheral and central compartments. The tracer 6-[18F]fluoro-L-dopa (FDOPA) is used here in positron emission tomography (PET) studies of Rhesus monkey brain in combination with the peripheral aromatic amino acid decarboxylase (AAAD) inhibitor carbidopa and the catechol-O-methyltrans-ferase (COMT) inhibitor tolcapone (Ro 40-7592).
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References
Zürcher G, Dingemanse J, Da Prada M. Potent COMT inhibition by Ro 40-7592 in the periphery and in the brain. Advances in Neurology 1993;60:641-647
Gjedde A, Reith J, Dyve S, et al. Dopa decarboxylase activity of the living human brain. Proc Natl Acad Sci U S A 1991;88:2721–2725
Cumming P, Léger GC, Kuwabara H, Gjedde A. Pharmacokinetics of plasma 6-[18F]Fluoro-L-3,4-dihydroxyphenylalanine ([18F]FDOPA) in humans. J Cereb Blood Flow Metab 1993;13:668–675
Patlak CS, Blasberg RG, Fenstermacher JD. Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake data. J Cereb Blood Flow Metab 1983;3:1–7
Günther I, Psylla M, Reddy GN, et al. PET in drug evaluation: influence of three different COMT inhibitors on peripheral [NCA] 6-[18F]fluoro-L-dopa metabolism in Rhesus monkey. Accepted Nuclear Medicine and Biology.
Psylla M, Günther I, Antonini A, et al. Cerebral 6-[18F]fluoro-L-dopa uptake in Rhesus monkey: pharmacological influence of aromatic amino acid decarboxylase (AAAD) and catechol-O-methyltransferase (COMT) inhibition. (submitted)
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© 1995 Springer Science+Business Media Dordrecht
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Karin, J., Leonhard, L.K., Ilonka, G., Maria, P. (1995). COMT Inhibition: Pharmacology of Tolcapone and 6-[18F]-Fluoro-L-DOPA (FDOPA) PET Results. In: Comar, D. (eds) PET for Drug Development and Evaluation. Developments in Nuclear Medicine, vol 26. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-0429-6_17
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DOI: https://doi.org/10.1007/978-94-011-0429-6_17
Publisher Name: Springer, Dordrecht
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