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AbstractAbstract
[en] The labeled serotonin agonist 3-[18F]fluoro-N-(α,α,α-trifluoro-m-tolyl)piperazine (18FTFMPP) was prepared rapidly using the labeling procedure for trifluorotoluenes, [18F]fluoro-for-nitro exchange, followed by an alumina-supported bis-alkylation. After normal-phase HPLC purification, the labeled product was obtained in 20-32% (n = 20) decay-corrected radiochemical yield with a radiochemical purity >98% and a specific activity of 100 GBq/μmol. The synthesis time including purification was 3 h. The receptor binding affinity of FTFMPP to rat brain membranes was found to be similar to that of the nonfluorinated parent compound (TFMPP). Although TFMPP has been proposed by others as an agent for the imaging of serotonin receptors, only minimal receptor-mediated uptake was observed
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Source
S0969805197000632; Copyright (c) 1997 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.; Country of input: International Atomic Energy Agency (IAEA)
Record Type
Journal Article
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AMINES, ANIMALS, AROMATICS, AUTONOMIC NERVOUS SYSTEM AGENTS, AZAARENES, AZINES, AZOLES, BETA DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, BODY, CELL CONSTITUENTS, CENTRAL NERVOUS SYSTEM, CHEMICAL REACTIONS, DRUGS, ELEMENTS, FLUORINE ISOTOPES, HETEROCYCLIC COMPOUNDS, HOURS LIVING RADIOISOTOPES, HYDROXY COMPOUNDS, INDOLES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, LIGHT NUCLEI, MAMMALS, MATERIALS, MEMBRANE PROTEINS, MEMBRANES, METALS, NANOSECONDS LIVING RADIOISOTOPES, NERVOUS SYSTEM, NEUROREGULATORS, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, ORGANS, PROTEINS, PYRAZINES, PYRROLES, RADIOACTIVE MATERIALS, RADIOISOTOPES, RADIOPROTECTIVE SUBSTANCES, RESPONSE MODIFYING FACTORS, RODENTS, SYMPATHOMIMETICS, TRYPTAMINES, VERTEBRATES
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