Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
In vivo imaging of serotonin transporters with [Tc-99m]TRODAT-1 in nonhuman primates
Autore:
Dresel, SHJ; Kung, MPT; Huang, XF; Plossl, K; Hou, C; Shiue, CY; Karp, J; 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:
EUROPEAN JOURNAL OF NUCLEAR MEDICINE
fascicolo: 4, volume: 26, anno: 1999,
pagine: 342 - 347
SICI:
0340-6997(199904)26:4<342:IVIOST>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
PHOTON EMISSION TOMOGRAPHY; NOR-BETA-CIT; HUMAN BRAIN; DOPAMINE TRANSPORTERS; PARKINSONS-DISEASE; MAJOR DEPRESSION; SITES; MCN5652; LIGAND; AGENTS;
Keywords:
brain; single-photon emission tomography; serotonin transporters; [Tc-99m]TRODAT-1;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
31
Recensione:
Indirizzi per estratti:
Indirizzo: Dresel, SHJ Univ Penn, Dept Radiol, 3700 Market St,Room 305, Philadelphia,PA 19104 USA Univ Penn 3700 Market St,Room 305 Philadelphia PA USA 19104 SA
Citazione:
S.H.J. Dresel et al., "In vivo imaging of serotonin transporters with [Tc-99m]TRODAT-1 in nonhuman primates", EUR J NUCL, 26(4), 1999, pp. 342-347

Abstract

[Tc-99m]TRODAT-1 was the first Tc-99m-labeled imaging agent to show specific binding to dopamine transporters (DAT) in the striatum (STR) of human brain. Additionally, in vitro binding and autoradiographic experiments demonstrated that this tracer also binds to serotonin transporters (SERT) in the midbrain/hypothalamus (MB) area. In this study, [Tc-99m]TRODAT-1 was investigated as a potentially useful ligand to image SEPT in the MB of living brain. A total of eight single-photon emission tomography (SPET) scans were performed in two baboons (Papio anubis) after intravenous (i.v.) injection of740 MBq (20 mCi) of [Tc-99m]TRODAT-1 using a triple-head gamma camera equipped with ultra-high-resolution fan-beam collimators (scan time: 0-210 min). In four blocking studies, baboons were pre-treated with (+)McN5652 (1 mg/kg, i.v.) or methylphenidate (1 mg/kg, i.v.) to specifically block SERT or DAT, respectively. After co-registration with magnetic resonance images of the same baboon, a region of interest analysis was performed using predefined templates to calculate specific uptake in the midbrain area and the striatum, with the cerebellum as the background region [(MB-CB)/CB, (STR-CB)/CB]. Additionally, two PET scans of the same baboons were performed after i.v, injections of 74-111 MBy (2-3 mCi) of [C-11](+)McN5652 to identify the SERT sites. In [Tc-99m]TRODAT-1/SPET scans, the SEPT sites in the MB region were clearly visualized. Semiquantitative analysis revealed a specific uptake in MB ([MB-CB]/CB) of 0.30+/-0.02, which was decreased to 0.040+/-0.005 after pretreatment with nonradioactive (+)McN5652. a selective SERT ligand. Pretreatment with methylphenidate reduced the specific binding of [Tc-99m]TRODAT-1 to DAT sites [(STR-CB)/CB] from 2.45+/-0.13 to 0.32+/-0.04 without any effect on its binding to SERT sites [(MB-CB)/CB], which was confirmed by the co-registration of the [C-11](+)McN5652/PET scans. This preliminary study suggests that specific binding of [Tc-99m]TRODAT-1 to SEPT sites can be detected by in vivo SPET imaging despite the low target to background ratio. These findings provide impetus for further development of similar compounds with improved binding affinity and selectivity to SERT sites.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 01:41:29