Document Detail

Striatal [18F]fluorodopa utilization after COMT inhibition with entacapone studied with PET in advanced Parkinson's disease.
MedLine Citation:
PMID:  9620057     Owner:  NLM     Status:  MEDLINE    
The effect of peripheral catechol-O-methyltransferase (COMT) inhibition with entacapone on striatal uptake of 6-[18F]fluoro-L-dopa (FDOPA) was studied with PET both without and with entacapone in fifteen advanced parkinsonian patients and six healthy controls. Entacapone significantly enhanced the fraction of unmetabolized FDOPA in plasma from 16% to about 50% at 80 minutes after FDOPA injection in all subjects. The striatal to occipital ratios and the striatal FDOPA uptake, expressed as a modified decarboxylation coefficient (k3R0), was significantly increased in healthy controls, whereas in parkinsonian patients the increase was significant only in the caudate. On the other hand, the influx constant (Ki) decreased significantly in the caudate and putamen in parkinsonian patients; in healthy controls the Ki remained virtually unchanged. Effective peripheral COMT inhibition markedly increased the fraction of FDOPA in plasma and thus its availability in the brain for decarboxylation both in patients and control subjects. However, the change in striatal FDOPA uptake was modest in the advanced parkinsonian patients as compared to that in control subjects, because of the advanced disease, decreased storage capacity, or both.
H M Ruottinen; J O Rinne; U H Ruotsalainen; J R Bergman; V J Oikonen; M T Haaparanta; O H Solin; A O Laihinen; U K Rinne
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Publication Detail:
Type:  Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of neural transmission. Parkinson's disease and dementia section     Volume:  10     ISSN:  0936-3076     ISO Abbreviation:  J Neural Transm Park Dis Dement Sect     Publication Date:  1995  
Date Detail:
Created Date:  1998-06-17     Completed Date:  1998-06-17     Revised Date:  2013-11-25    
Medline Journal Info:
Nlm Unique ID:  8914371     Medline TA:  J Neural Transm Park Dis Dement Sect     Country:  AUSTRIA    
Other Details:
Languages:  eng     Pagination:  91-106     Citation Subset:  IM    
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MeSH Terms
Aged, 80 and over
Analysis of Variance
Catechol O-Methyltransferase / antagonists & inhibitors*
Catechols / pharmacology*
Corpus Striatum / drug effects*,  radionuclide imaging*
Dihydroxyphenylalanine / analogs & derivatives*,  diagnostic use,  metabolism
Enzyme Inhibitors / pharmacology*
Middle Aged
Parkinson Disease / radionuclide imaging*
Tomography, Emission-Computed
Reg. No./Substance:
0/Catechols; 0/Enzyme Inhibitors; 0/Nitriles; 2C598205QX/fluorodopa F 18; 4975G9NM6T/entacapone; 63-84-3/Dihydroxyphenylalanine; EC O-Methyltransferase

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