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Titolo:
TC-99M-LABELED TROPANES AS DOPAMINE TRANSPORTER IMAGING AGENTS
Autore:
MEEGALLA S; PLOSSL K; KUNG MP; CHUMPRADIT S; STEVENSON DA; FREDERICK D; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104
Titolo Testata:
Bioconjugate chemistry
fascicolo: 4, volume: 7, anno: 1996,
pagine: 421 - 429
SICI:
1043-1802(1996)7:4<421:TTADTI>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; TECHNETIUM COMPLEXES; PARKINSONS-DISEASE; OXOMETAL COMPLEXES; RECEPTOR-BINDING; LIGANDS; AFFINITY; RHENIUM(V); SITES; COORDINATION;
Tipo documento:
Article
Natura:
Periodico
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
S. Meegalla et al., "TC-99M-LABELED TROPANES AS DOPAMINE TRANSPORTER IMAGING AGENTS", Bioconjugate chemistry, 7(4), 1996, pp. 421-429

Abstract

The development of novel Tc-99m-labeled tropane derivatives as dopamine transporter imaging agents is reported. A series of neutral and lipophilic conjugated complexes, containing N-(alkylthiolato)tropane, aminobis(ethylthiolato), and a [(TC)-T-99m]TcO3+ center core, were prepared and evaluated as central nervous system (CNS) dopamine transporter imaging agents in rats. One of the compounds, [Tc-99m]technetium, [methyl oxylato-S][[2,2'-(methylimino)bis[ethanethiolato]] (2-)-N,S,S']oxo(25), displayed low initial uptake in rat brain (0.1% at 2 min post iv injection); the striatal/cerebellar (ST/CB) ratio reached 3.50 at 60min after an iv injection. The specific uptake can be blocked by pretreating rats with a competing dopamine transporter binding agent, beta-CIT (RTI-55, N-methyl-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane; iv; 1 mg/kg), which reduced the regional brain uptake ratio (ST/CB)to 1.0. In contrast, the specific uptake in striatum was not affectedby pretreating rats with a noncompeting ligand, haldol (iv, 1 mg/kg). In vitro autoradiography of rat brain sections exhibited elevated labeling in striatum, major islands of Calleja, and olfactory tubercle regions, where dopamine neurons are known to be concentrated. This series of compounds is the first example of technetium-99m labeled CNS receptor-specific imaging agents and may provide a convenient source of short-lived imaging agents for routine diagnosis of CNS abnormality in conjunction with single photon emission computed tomography.

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Documento generato il 18/01/20 alle ore 10:42:29