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Titolo:
Tc-99m-labeled MIBG derivatives: Novel Tc-99m complexes as myocardial imaging agents for sympathetic neurons
Autore:
Zhuang, ZP; Kung, MP; Mu, M; Hou, A; Kung, HF;
Indirizzi:
Univ Penn, Dept Radiol, Philadelphia, PA 19104 USA Univ Penn PhiladelphiaPA USA 19104 pt Radiol, Philadelphia, PA 19104 USA Univ Penn, Dept Pharmacol, Philadelphia, PA 19104 USA Univ Penn Philadelphia PA USA 19104 Pharmacol, Philadelphia, PA 19104 USA
Titolo Testata:
BIOCONJUGATE CHEMISTRY
fascicolo: 2, volume: 10, anno: 1999,
pagine: 159 - 168
SICI:
1043-1802(199903/04)10:2<159:TMDNTC>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
METAIODOBENZYLGUANIDINE UPTAKE; TECHNETIUM-99M L,L-ECD; NOREPINEPHRINE; TRANSPORTERS; DOPAMINE; BIODISTRIBUTION; HUMANS; ANALOG; HEART;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Kung, HF Univ Penn, Dept Radiol, 3700 Market St,Room 305, Philadelphia, PA19104 USA Univ Penn 3700 Market St,Room 305 Philadelphia PA USA 19104 4 USA
Citazione:
Z.P. Zhuang et al., "Tc-99m-labeled MIBG derivatives: Novel Tc-99m complexes as myocardial imaging agents for sympathetic neurons", BIOCONJ CHE, 10(2), 1999, pp. 159-168

Abstract

Radioactive-iodine-labeled meta-iodobenzylguanidine (MIBG) is currently being used as an in vivo imaging agent to evaluate neuroendocrine tumors as well as the myocardial sympathetic nervous system in patients with myocardial infarct and cardiomyopathy. It is generally accepted that MIBC; is an analogue of norepinephrine and its uptake in the heart corresponds to the distribution of norepinephrine and the density of sympathetic neurons. A seriesof MIBG derivatives containing suitable chelating functional groups N2S2 for the formation of [(TcO)-O-v]3+N2S2 complex was successfully synthesized,and the Tc-99m-labeled complexes were prepared and tested in rats. One of the compounds, [Tc-99m]2, tested showed significant, albeit lower, heart uptakes post iv injection in rats (0.21% dose/g at 4 h) as compared to [I-125]MIBG (1.7% dose/g at 4 h). The heart uptake of the Tc-99m-labeled complex appears to be specific and can be reduced by co-injection with nonradioactive MIBG or by pretreatment with desipramine, a selective norepinephrine transporter inhibitor. Further evaluation of the in vitro uptake of [Tc-99m]2 in cultured neuroblastoma cells displayed consistently lower, but measurable uptake (approximately 10% of that for [I-125]MIBG). These preliminary results suggested that the mechanisms of heart uptake of [Tc-99m]2 may be related to those for [I-125]MIBG uptake. If suitable Tc-99m-labeled MIBG derivatives can be further developed, the prevalent availability of Tc-99m in nuclear medicine clinics will allow them to be readily available for widespread application.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 03:16:58