| The effect of ring-fluorination on the rate of O-methylation of dihydroxyphenylalanine (DOPA) by catechol-O-methyltransferase: significance in the development of 18F-PETT scanning agents. | |
| | |
MedLine Citation:
|
PMID: 3927916 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
The three ring-fluorinated analogs of dihydroxyphenylalanine (DOPA) were synthesized and the kinetics of their O-methylation catalyzed by catechol-O-methyltransferase compared to those of DOPA. The affinities (Km) of 2-FDOPA, 5-FDOPA, DOPA, and 6-FDOPA were 20, 23, 55, and 552 microM, respectively, whilst the Vmax values were 4.0, 4.4, 5.0 and 5.4 nmol per min per mg protein. The importance of the low affinity and decreased rate constant of 6-FDOPA for COMT are discussed with regard to the use of 6-FDOPA as an 18-fluorine labeled probe for positron emission transaxial tomography (PETT). |
| | |
Authors:
|
C R Creveling; K L Kirk |
Related Documents
:
|
410006 - Use of aurintricarboxylic acid as an inhibitor of nucleases during nucleic acid isolation. 17443886 - Chemical etiology of nucleic acids: aminopropyl nucleic acids (apnas). 8914986 - Inhibitor/fatty acid interactions with cytochrome p-450 bm3. 17150706 - Development of real time imaging of specific messenger rna in a living cell using artif... 20017486 - Phenolic and short-chained aliphatic organic acid constituents of wild oat (avena fatua... 18939836 - Synthesis and degradation of nucleic acid components by formamide and iron sulfur miner... |
Publication Detail:
|
Type: Comparative Study; Journal Article |
Journal Detail:
|
Title: Biochemical and biophysical research communications Volume: 130 ISSN: 0006-291X ISO Abbreviation: Biochem. Biophys. Res. Commun. Publication Date: 1985 Aug |
Date Detail:
|
Created Date: 1985-09-25 Completed Date: 1985-09-25 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 0372516 Medline TA: Biochem Biophys Res Commun Country: UNITED STATES |
Other Details:
|
Languages: eng Pagination: 1123-31 Citation Subset: IM |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Catechol O-Methyltransferase / metabolism* Dihydroxyphenylalanine / analogs & derivatives*, chemical synthesis, metabolism* Fluorine Kinetics Liver / enzymology Methylation Radioisotopes Rats Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
|
0/Radioisotopes; 63-84-3/Dihydroxyphenylalanine; 7782-41-4/Fluorine; EC 2.1.1.6/Catechol O-Methyltransferase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Differential effect of external calcium on the oxygenated metabolism of endogenous and exogenous ara...
Next Document: Stimulation of the cyclic AMP-dependent protein kinase-catalyzed phosphorylation of phosphorylase ki...