Positron emission tomography in drug evaluation: Influence of three different catechol- O-methyltransferase inhibitors on metabolism of [NCA] 6-[ 18F]fluoro- l-dopa in rhesus monkey

We compared the influence of three different catechol- O-methyltransferase (COMT) inhibitors (CGP 28014, OR-611 and Ro 40–7592) on the metabolism of no-carrier-added (NCA) 6-[ 18F]fluoro- l-dopa (6-FDOPA) in one Rhesus monkey. All three COMT inhibitors improved 6-FDOPA availability in plasma, increa...

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Published in:Nuclear medicine and biology 1995-10, Vol.22 (7), p.921-927
Main Authors: Günther, I., Psylla, M., Reddy, G.N., Antonini, A., Vontobel, P., Reist, H.W., Zollinger, A., Nickles, R.J., Beer, H.-F., Schubiger, P.A., Leenders, K.L.
Format: Article
Language:English
Subjects:
Amidines - pharmacokinetics
Amidines - pharmacology
Animals
Benzophenones - pharmacokinetics
Benzophenones - pharmacology
Biological Availability
Brain - drug effects
Brain - enzymology
Brain - metabolism
Catechol O-Methyltransferase Inhibitors
Catechols - pharmacokinetics
Catechols - pharmacology
Dihydroxyphenylalanine - analogs & derivatives
Dihydroxyphenylalanine - metabolism
Dihydroxyphenylalanine - pharmacokinetics
Drug Evaluation, Preclinical - methods
Enzyme Inhibitors - pharmacokinetics
Enzyme Inhibitors - pharmacology
Female
Fluorine Radioisotopes
Macaca mulatta
Nitriles
Nitrophenols
Pyridones - pharmacokinetics
Pyridones - pharmacology
Tomography, Emission-Computed
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Summary:We compared the influence of three different catechol- O-methyltransferase (COMT) inhibitors (CGP 28014, OR-611 and Ro 40–7592) on the metabolism of no-carrier-added (NCA) 6-[ 18F]fluoro- l-dopa (6-FDOPA) in one Rhesus monkey. All three COMT inhibitors improved 6-FDOPA availability in plasma, increased the specific uptake in the brain and thus improved 6-FDOPA uptake measurements using positron emission tomography (PET). Best results were obtained with Ro 40–7592.
ISSN:0969-8051
1872-9614
DOI:10.1016/0969-8051(95)00032-S