Abstract
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.
MeSH terms
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3,4-Dihydroxyphenylacetic Acid / metabolism
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Amidines / pharmacology*
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Catechol O-Methyltransferase Inhibitors*
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Dihydroxyphenylalanine / metabolism
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Homovanillic Acid / metabolism
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Humans
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Male
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Pyridones / pharmacology*
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Tyrosine / analogs & derivatives*
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Tyrosine / biosynthesis
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Tyrosine / blood
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Tyrosine / pharmacokinetics
Substances
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Amidines
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Catechol O-Methyltransferase Inhibitors
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Pyridones
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3,4-Dihydroxyphenylacetic Acid
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N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine
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Tyrosine
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Dihydroxyphenylalanine
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3-methoxytyrosine
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Homovanillic Acid