Filters
Results 1 - 1 of 1
Results 1 - 1 of 1.
Search took: 0.016 seconds
AbstractAbstract
[en] Both FLB 457 and FLB 463, two substituted benzamides with high affinity for the dopamine D-2 receptors, were labeled with bromine-76 for PET investigations. [76Br]FLB 457 was prepared by electrophilic substitution of the tributyltin precursor. The radiochemical yield was 80%. [76Br]FLB 463 was prepared by a direct electrophilic substitution enhanced by the hydroxyl group of the debromo analogue, with a total radiochemical yield of 50%. Radiochemical and chemical purity values of the radioligands as analyzed by radio-TLC and HPLC were >99%, and the specific radioactivity was ∼40 GBq/μmol. During PET examinations of [76Br]FLB 457 and [76Br]FLB 463 binding in baboons there was a rapid and high uptake in the striatum. The striatal radioactivity concentration reached a plateau 1 h postinjection (p.i.). The striatum-to-cerebellum radioactivity concentration ratio increased from 11 at 1 p.i., to 28 at 4 h p.i. for [76Br]FLB 457, owing to a continuous wash-out from the cerebellum. For [76Br]FLB 463 the corresponding value increased from 10 to 19.5. [76Br]FLB 457 has in contrast to [76Br]FLB 463 a high uptake in thalamic structures and has therefore an additional potential as a radioligand for PET examination of extrastriatal dopamine D-2 receptors in the living human brain
Primary Subject
Source
0969805196000789; Copyright (c) 1996 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.; Country of input: International Atomic Energy Agency (IAEA)
Record Type
Journal Article
Journal
Country of publication
AMINES, ANIMALS, AROMATICS, AUTONOMIC NERVOUS SYSTEM AGENTS, BETA DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, BODY, BRAIN, BROMINE ISOTOPES, CARDIOTONICS, CARDIOVASCULAR AGENTS, CENTRAL NERVOUS SYSTEM, COMPUTERIZED TOMOGRAPHY, DIAGNOSTIC TECHNIQUES, DRUGS, ELECTRON CAPTURE RADIOISOTOPES, EMISSION COMPUTED TOMOGRAPHY, HOURS LIVING RADIOISOTOPES, HYDROXY COMPOUNDS, INTERMEDIATE MASS NUCLEI, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, MAMMALS, MEMBRANE PROTEINS, MONKEYS, NERVOUS SYSTEM, NEUROREGULATORS, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANS, PHENOLS, POLYPHENOLS, PRIMATES, PROTEINS, RADIOISOTOPES, SECONDS LIVING RADIOISOTOPES, SYMPATHOMIMETICS, TOMOGRAPHY, VERTEBRATES
Reference NumberReference Number
INIS VolumeINIS Volume
INIS IssueINIS Issue