Document Detail

Effect of the new selective COMT inhibitor CGP 28014 A on the formation of 3-O-methyldopa (3OMD) in plasma of healthy subjects.
MedLine Citation:
PMID:  2128511     Owner:  NLM     Status:  MEDLINE    
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.
P R Bieck; E Nilsson; K H Antonin
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of neural transmission. Supplementum     Volume:  32     ISSN:  0303-6995     ISO Abbreviation:  J. Neural Transm. Suppl.     Publication Date:  1990  
Date Detail:
Created Date:  1991-05-29     Completed Date:  1991-05-29     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0425126     Medline TA:  J Neural Transm Suppl     Country:  AUSTRIA    
Other Details:
Languages:  eng     Pagination:  387-91     Citation Subset:  IM    
Human Pharmacology Institute, Ciba-Geigy GmbH, Tübingen, Federal Republic of Germany.
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MeSH Terms
3,4-Dihydroxyphenylacetic Acid / metabolism
Amidines / pharmacology*
Catechol O-Methyltransferase / antagonists & inhibitors*
Dihydroxyphenylalanine / metabolism
Homovanillic Acid / metabolism
Pyridones / pharmacology*
Tyrosine / analogs & derivatives*,  biosynthesis,  blood,  pharmacokinetics
Reg. No./Substance:
0/Amidines; 0/Pyridones; 102-32-9/3,4-Dihydroxyphenylacetic Acid; 111757-17-6/N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine; 306-08-1/Homovanillic Acid; 55520-40-6/Tyrosine; 63-84-3/Dihydroxyphenylalanine; 7636-26-2/3-methoxytyrosine; EC O-Methyltransferase

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