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AbstractAbstract
[en] Bromolisuride, an ergoline derivative, was labeled with the positron emitter radionuclide, bromine 76. In vitro and in vivo binding and competition studies in rats demonstrated a high affinity (KD = 0.3 nM) and a high specificity of this new radioligand for D-2 dopamine receptors. PET kinetic studies in baboons showed an accumulation of [76Br]bromolisuride in the striatum which reached a maximum 30 min post-injection and which could be displaced by haloperidol. All these results indicated that this new ligand is certainly suitable for the non-invasive in vivo quantitative imaging of D-2 dopamine receptor sites in humain brain. (Auth.)
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20 refs.; 6 figs.; 1 table.
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Journal Article
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AMINES, ANIMALS, AROMATICS, BETA DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, BODY, BROMINE ISOTOPES, CARDIOTONICS, CARDIOVASCULAR AGENTS, CENTRAL NERVOUS SYSTEM, COMPUTERIZED TOMOGRAPHY, DRUGS, ELECTRON CAPTURE RADIOISOTOPES, EMISSION COMPUTED TOMOGRAPHY, HOURS LIVING RADIOISOTOPES, HYDROXY COMPOUNDS, INTERMEDIATE MASS NUCLEI, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, MAMMALS, MONKEYS, NERVOUS SYSTEM, NEUROREGULATORS, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANIC HALOGEN COMPOUNDS, ORGANS, PHENOLS, POLYPHENOLS, PRIMATES, RADIOISOTOPES, RODENTS, SECONDS LIVING RADIOISOTOPES, STEROIDS, SYMPATHOMIMETICS, TOMOGRAPHY, VERTEBRATES
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