Development of N-[3-(2',4'-dichlorophenoxy)-2-18F-fluoropropyl]-N-methylpropargylamine (18F-fluoroclorgyline) as a potential PET radiotracer for monoamine oxidase-A
Mukherjee, Jogeshwar; Yang, Z.-Y., E-mail: jogeshwar_mukherjee@ketthealth.com1999
AbstractAbstract
[en] We have synthesized N-[3-(2',4'-dichlorophenoxy)-2-18F-fluoropropyl]-N-methylpropargylamine (18F-fluoroclorgyline) as a potential positron emission tomography (PET) radiotracer for monoamine oxidase A (MAO-A). The radiosynthesis was carried out by a 18F-fluoride-for-mesylate substitution reaction in approximately 20% radiochemical yield in specific activities of 1-2 Ci/μmol. Selectivity for MAO-A was demonstrated by the high affinity of clorgyline ( IC50=39 nM) and lower affinity of (R)-deprenyl ( IC50≥100 μM) for the inhibition of 18F-fluoroclorgyline binding in vitro in rat brain membranes. The uptake of 18F-fluoroclorgyline in the rat brains was high (>1.0% injected dose/g). The binding of 18F-fluoroclorgyline in the rat brain correlated with the distribution of MAO-A and was inhibited by preadministration of MAO-A inhibitors, clorgyline, and Ro 41-1049, whereas (R)-deprenyl, a MAO-B blocker, had no inhibitory effect. These results suggest that 18F-fluoroclorgyline is a potential PET radiotracer for MAO-A
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S096980519900027X; Copyright (c) 1999 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.; Country of input: Bulgaria
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ALKYL RADICALS, BETA DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, BODY, CENTRAL NERVOUS SYSTEM, COMPUTERIZED TOMOGRAPHY, DIAGNOSTIC TECHNIQUES, EMISSION COMPUTED TOMOGRAPHY, ENZYMES, FLUORINE ISOTOPES, HOURS LIVING RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPE APPLICATIONS, ISOTOPES, LIGHT NUCLEI, NERVOUS SYSTEM, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANS, OXIDOREDUCTASES, PROTEINS, RADICALS, RADIOACTIVITY LOGGING, RADIOISOTOPES, TOMOGRAPHY, TRACER TECHNIQUES, WELL LOGGING
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