Comparative in vivo metabolism of 6-[18F]fluoro-L-dopa and [3H]L-dopa in rats

Biochemical Pharmacology
W P MelegaJ R Barrio

Abstract

In vivo double-label experiments in rats were designed to correlate the peripheral and cerebral metabolism of 6-[18F]fluoro-L-DOPA [( 18F]FDOPA) with that of [3H]L-DOPA. Authentic samples of the major [18F]FDOPA metabolites were synthesized to identify the 18F-labeled metabolites. After carbidopa pretreatment and intravenous administration of the compound, the products of peripheral metabolism in plasma were analyzed at times from 3 to 60 min. In the periphery, amine conjugates were detected but they accounted for less than 15% of the total radioactivity; the major metabolites were 3-O-methyl-6-[18F]fluoro-L-DOPA and 3-O-methyl-[3H]L-DOPA. The rate and extent of 3-O-methylation of [18F]FDOPA exceeded that of [3H]L-DOPA. Both 3-O-methylated products entered the striatum and cerebellum where they contributed significant but uniform activity. Analysis of cerebral metabolism in these structures indicated a linear accumulation of total radioactivity: a striatum/cerebellum ratio of 2 was observed by 60 min. 6-[18F]Fluorodopamine (35%) and [3H]dopamine (55%) were the major metabolites formed in the striatum: however, the methylated [18F]FDOPA and [3H]DOPA products of predominantly peripheral origin represented 55% (18F) and 35% (3H) o...Continue Reading

References

Dec 1, 1979·Journal of Medicinal Chemistry·K L KirkC R Creveling
Nov 16, 1979·Brain Research·L C Murrin, M J Kuhar
Jan 1, 1978·Biochemical Pharmacology·T R BosinR P Maickel
Jan 1, 1988·Annual Review of Pharmacology and Toxicology·J R BarrioM E Phelps
Feb 1, 1987·Journal of Neurochemistry·P CummingE G McGeer
Apr 1, 1987·Journal of Neurochemistry·G FirnauE S Garnett
May 23, 1985·Neuroscience Letters·A C MichaelD B Neill
Jan 1, 1983·Molecular and Cellular Biochemistry·J M Masserano, N Weiner
Apr 1, 1984·Medicinal Research Reviews·K L Kirk, C R Creveling
Aug 15, 1983·Life Sciences·S E Shoaf, M A Elchisak

❮ Previous
Next ❯

Citations

Jan 1, 1996·Movement Disorders : Official Journal of the Movement Disorder Society·C RaftopoulosJ Hildebrand
Jan 1, 1991·Journal of Neural Transmission. General Section·P HartvigB Långström
Jan 1, 1995·Journal of Neural Transmission. General Section·S DethyS Goldman
Jan 1, 1995·Journal of Neural Transmission. Parkinson's Disease and Dementia Section·H M RuottinenU K Rinne
Mar 1, 1993·Journal of the Neurological Sciences·D J Brooks
Jan 1, 1990·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·M PerlmutterJ R Barrio
Aug 1, 1992·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·D MuraliR J Nickles
Mar 1, 1993·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·M NamavariJ R Barrio
Dec 7, 2002·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·K L Leenders
May 9, 2000·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·N HaradaH Tsukada
Jul 1, 1996·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J R BarrioM E Phelps
Oct 26, 1999·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·R TorstensonB Långström
Jun 9, 1998·Annals of the New York Academy of Sciences·P CummingA Gjedde
May 6, 2009·The AAPS Journal·Eric D Agdeppa, Mary E Spilker
Jul 1, 2008·PET Clinics·Vikas PrasadRichard P Baum
Aug 1, 1997·Biochemical Pharmacology·J R BarrioM E Phelps
Dec 6, 2008·Schizophrenia Research·Shoko NozakiTetsuya Suhara
Oct 1, 2013·Nuclear Medicine and Biology·Michael R Kilbourn
Jul 25, 2000·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·K Shoghi-JadidJ R Barrio
Jul 1, 1993·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·P CummingA Gjedde
Nov 1, 1991·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·S C HuangM E Phelps
Nov 1, 1991·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·W P MelegaJ R Barrio

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.