title: 3-O-methyldopa administration does not alter fluorodopa transport into the brain.
abstract: To determine if 3-O-methyldopa (3OMD) significantly inhibits the transport of 6-[18F]fluorodopa (6-FD) into the brain at the concentration normally encountered during L-dopa administration, we performed 6-FD studies with positron emission tomography in cynomolgus monkeys in the presence and absence of 3OMD. Infusion of 3OMD was designed to produce plasma concentrations equivalent to those seen in patients on chronic L-dopa therapy. Plasma 3OMD levels of 39 +/- 4 microM did not alter the blood-brain transfer rate of 6-FD. 6-FD positron emission tomographic studies in parkinsonian patients will therefore not be altered by 3OMD present in the blood in those patients taking L-dopa preparations. These results do not support the hypothesis that transport of L-dopa into the brain is inhibited by 3OMD to cause the declining response seen in patients with advanced Parkinson's disease.
authors.affiliation: Department of Neurology and Neurosurgery, McGill University, Montreal, Quebec, Canada.
authors.forename: M
authors.initials: M
authors.lastname: Guttman
authors.forename: G
authors.initials: G
authors.lastname: Léger
authors.forename: J M
authors.initials: JM
authors.lastname: Cedarbaum
authors.forename: A
authors.initials: A
authors.lastname: Reches
authors.forename: W
authors.initials: W
authors.lastname: Woodward
authors.forename: A
authors.initials: A
authors.lastname: Evans
authors.forename: M
authors.initials: M
authors.lastname: Diksic
authors.forename: A
authors.initials: A
authors.lastname: Gjedde
mesh_terms: D026905:Amino Acid Transport Systems; D000596:Amino Acids / Q000097:blood; D000818:Animals; D001667:Binding, Competitive; D001692:Biological Transport / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000187:drug effects*; D001921:Brain / Q000000981:diagnostic imaging*; D002352:Carrier Proteins / Q000378:metabolism*; D004295:Dihydroxyphenylalanine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008252:Macaca fascicularis; D008297:Male; D014055:Tomography, Emission-Computed / Q000379:methods*; D014443:Tyrosine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D026905:Amino Acid Transport Systems; D000596:Amino Acids; D002352:Carrier Proteins; C043437:fluorodopa F 18; D014443:Tyrosine; D004295:Dihydroxyphenylalanine; C008404:3-methoxytyrosine