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, 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.
Günther
I
I
PET Department, Paul Scherrer Institute, Villigen PSI, Switzerland.
Psylla
M
M
Reddy
G N
GN
Antonini
A
A
Vontobel
P
P
Reist
H W
HW
Zollinger
A
A
Nickles
R J
RJ
Beer
H F
HF
Schubiger
P A
PA
D000578:Amidines / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001577:Benzophenones / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D001921:Brain / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D065098:Catechol O-Methyltransferase Inhibitors; D002396:Catechols / Q000493:pharmacokinetics / Q000494:pharmacology; D004295:Dihydroxyphenylalanine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D005260:Female; D005462:Fluorine Radioisotopes; D008253:Macaca mulatta; D009570:Nitriles; D009596:Nitrophenols; D011728:Pyridones / Q000493:pharmacokinetics / Q000494:pharmacology; D000077867:Tolcapone; D014055:Tomography, Emission-Computed
D000578:Amidines; D001577:Benzophenones; D065098:Catechol O-Methyltransferase Inhibitors; D002396:Catechols; D004791:Enzyme Inhibitors; D005462:Fluorine Radioisotopes; D009570:Nitriles; D009596:Nitrophenols; D011728:Pyridones; C067181:N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine; C043437:fluorodopa F 18; C071192:entacapone; D004295:Dihydroxyphenylalanine; D000077867:Tolcapone