Effect of the new selective COMT inhibitor CGP 28014 A on the formation of 3-O-methyldopa (3OMD) in plasma of healthy subjects.
CGP 28014 A is a specific inhibitor of catechol-O-methyl transferase (COMT). The effect on COMT was assessed with the levodopa test in 5 unmedicated subjects and after pretreatment with 200-600 mg CGP 28014 p.o. Plasma concentrations of DOPA, 3-O-methyldopa (3OMD), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid were measured. CGP 28014 A decreased 3OMD not dose-related by 67% (p less than 0.05). This, and an increase of DOPAC shows COMT inhibition by this compound in humans.
Bieck
P R
PR
Human Pharmacology Institute, Ciba-Geigy GmbH, Tübingen, Federal Republic of Germany.
Nilsson
E
E
Antonin
K H
KH
D015102:3,4-Dihydroxyphenylacetic Acid / Q000378:metabolism; D000578:Amidines / Q000494:pharmacology*; D065098:Catechol O-Methyltransferase Inhibitors; D004295:Dihydroxyphenylalanine / Q000378:metabolism; D006719:Homovanillic Acid / Q000378:metabolism; D006801:Humans; D008297:Male; D011728:Pyridones / Q000494:pharmacology*; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000096:biosynthesis / Q000097:blood / Q000493:pharmacokinetics
D000578:Amidines; D065098:Catechol O-Methyltransferase Inhibitors; D011728:Pyridones; D015102:3,4-Dihydroxyphenylacetic Acid; C067181:N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine; D014443:Tyrosine; D004295:Dihydroxyphenylalanine; C008404:3-methoxytyrosine; D006719:Homovanillic Acid