Published August 15, 1985
| Version v1
Journal article
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
Description
The three ring-fluorinated analogs of dihydroxyphenylalanine (DOPA) were synthesized and the kinetics of their O-methylation catalyzed by catechol-O-methyltransferase (comt) 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)
Additional details
Publishing Information
- Journal Title
- Biochem. Biophys. Res. Commun.
- Journal Issue
- no.3
- Series
- Biochem. Biophys. Res. Commun.
- ISSN
- 0006-291X
- CODEN
- BBRCA
INIS
- Country of Publication
- United States
- Country of Input or Organization
- United States
- INIS RN
- 17036058
- Subject category
- S62: RADIOLOGY AND NUCLEAR MEDICINE;
- Descriptors DEI
- BIOCHEMISTRY; CHEMICAL PREPARATION; DOPA; FLUORINATION; FLUORINE 18; KINETICS; LIVER; METHYLATION; POSITRON COMPUTED TOMOGRAPHY; RADIOPHARMACEUTICALS; RATS; TRANSFERASES
- Descriptors DEC
- AMINO ACIDS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENT; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; BODY; CARBOXYLIC ACIDS; CHEMICAL REACTIONS; CHEMISTRY; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; DIGESTIVE SYSTEM; DRUGS; EMISSION COMPUTED TOMOGRAPHY; ENZYMES; FLUORINE ISOTOPES; GLANDS; HALOGENATION; HOURS LIVING RADIOISOTOPES; HYDROXY ACIDS; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; MAMMALS; MATERIALS; NEUROREGULATORS; NUCLEI; ODD-ODD NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANS; RADIOACTIVE MATERIALS; RADIOISOTOPES; RODENTS; SYNTHESIS; TOMOGRAPHY; VERTEBRATES