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Titolo:
PHARMACOLOGICAL EFFECTS OF DOPAMINERGIC DRUGS ON IN-VIVO BINDING OF [TC-99M]TRODAT-1 TO THE CENTRAL DOPAMINE TRANSPORTERS IN RATS
Autore:
DRESEL SHJ; KUNG MP; PLOSSL K; MEEGALLA SK; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104
Titolo Testata:
European journal of nuclear medicine
fascicolo: 1, volume: 25, anno: 1998,
pagine: 31 - 39
SICI:
0340-6997(1998)25:1<31:PEODDO>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; I-123 BETA-CIT; LIVING HUMAN BRAIN; IN-VIVO; SEROTONIN TRANSPORTERS; PARKINSONS-DISEASE; NONHUMAN-PRIMATES; BABOON BRAIN; LABELED 2-BETA-CARBOMETHOXY-3-BETA-(4-IODOPHENYL)TROPANE; INVIVO MICRODIALYSIS;
Keywords:
BRAIN; PARKINSONS DISEASE; DOPAMINE TRANSPORTER LIGANDS; SINGLE-PHOTON EMISSION TOMOGRAPHY; IN VIVO BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
73
Recensione:
Indirizzi per estratti:
Citazione:
S.H.J. Dresel et al., "PHARMACOLOGICAL EFFECTS OF DOPAMINERGIC DRUGS ON IN-VIVO BINDING OF [TC-99M]TRODAT-1 TO THE CENTRAL DOPAMINE TRANSPORTERS IN RATS", European journal of nuclear medicine, 25(1), 1998, pp. 31-39

Abstract

The put-pose of this study was to investigate the influence of drugs competing for the dopamine transporter (DAT) or changing intra- and/orextracellular dopamine levels on the binding of a novel technetium-99m labeled tropane derivative, technetium, [2-[[2-[[[3-(4-chlorophenyl)-8-methyl-8-azabicyclo [3, 2, 1]oct-2-yl]methyl] ethyl]amino]ethanethiolato(3)]-oxo-[1R-(exo-exo)]- [Tc-99m]TRODAT-1, to DAT. This paper describes the further characterization of [Tc-99m]TRODAT-1 binding sites in rats under conditions which may exist in patients receiving variousdrug treatments. All experiments were carried out using an i.v. injection of [Tc-99m]TRODAT-1 into male Sprague-Dawley rats. Measurements of % dose/gram ratio of (striatum-cerebellum)/cerebellum at 1 h post injection were used as an indicator for specific DAT binding. The biodistribution studies were performed in the presence of drugs which compete for the binding site, such as CFT (WIN 35,428) and methylphenidate, drugs which influence dopamine levels, such as L-DOPA, gamma-hydroxybutyrolactone, and alpha-methyl-p-tyrosine, and d-amphetamine, which both acts as a competitor for DAT binding and increases dopamine levels. Additionally, the influence of dopamine receptor agonists, such as apomorphine and (+)bromocriptine, on biodistribution was tested. Binding of [Tc-99m]TRODAT-1 to DAT was found to be inhibited by CFT, methylphenidate, and d-amphetamine in a dose-dependent manner. The specific binding of [Tc-99m]TRODAT-1 was not altered by dopamine receptor agonistsor by drugs which cause minor changes in dopamine levels. When administered in high doses (634 mu mol/kg), L-DOPA also decreased the binding of [Tc-99m]TRODAT-1. It is likely that a low dose of L-DOPA (normally needed in the treatment of Parkinson's disease) will not affect the results on [Tc-99m]TRODAT-1 single-photon emission tomographic (SPET) imaging studies. In conclusion, the results clearly demonstrate the specificity of [Tc-99m]TRODAT-1 binding to DAT in vivo. Competition for [Tc-99m]TRODAT-1 binding was observed only with drug treatment that significantly increases dopamine levels or actively competes for bindingat DAT. The results suggest that prior knowledge of whether patients are receiving various drug treatments may assist in the interpretationof DAT status as assessed by SPET imaging studies using [Tc-99m]TRODAT-1.

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Documento generato il 19/01/20 alle ore 09:27:49