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pubmed-article:8341294pubmed:abstractTextL-Dopa is metabolized to 3-O-methyldopa (3OMD) by catechol-O-methyltransferase (COMT). This reduces the amount of L-dopa available for entry into brain. We studied the effect of OR-611, a new COMT inhibitor, on plasma and brain 6-[18F]-fluoro-L-dopa (6FD) metabolism in cynomolgus monkeys with positron emission tomography (PET). OR-611 pretreatment substantially reduced plasma 6FD metabolism to 3-O-methylfluorodopa (3OMFD). PET measurements of striatal 6FD concentrations showed an average 2.3-fold increase following OR-611 pretreatment, compared to the same animals in the control state. OR-611 inhibits plasma metabolism of 6FD and increases brain uptake of this L-dopa analog. OR-611 appears to be a promising agent as an adjunct to L-dopa for the treatment of patients with Parkinson's disease.lld:pubmed
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pubmed-article:8341294pubmed:dateRevised2007-11-15lld:pubmed
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pubmed-article:8341294pubmed:articleTitleAdministration of the new COMT inhibitor OR-611 increases striatal uptake of fluorodopa.lld:pubmed
pubmed-article:8341294pubmed:affiliationMcConnell Brain Imaging Centre, Department of Neurology and Neurosurgery, McGill University, Montreal, Quebec, Canada.lld:pubmed
pubmed-article:8341294pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:8341294pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed