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Titolo:
An improved kit formulation of a dopamine transporter imaging agent: [Tc-99m]TRODAT-1
Autore:
Choi, SR; Kung, MP; Plossl, K; Meegalla, S; 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:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 4, volume: 26, anno: 1999,
pagine: 461 - 466
SICI:
0969-8051(199905)26:4<461:AIKFOA>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-CIT; PRIMATE BRAIN; SPECT; DOSIMETRY; BIODISTRIBUTION; RADIOLIGAND; ALTROPANE; TRODAT-1; AFFINITY; ANALOGS;
Keywords:
SPECT; dopamine transporter; kit formulation; Tc-99m radiopharmaceuticals; brain imaging;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
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:
S.R. Choi et al., "An improved kit formulation of a dopamine transporter imaging agent: [Tc-99m]TRODAT-1", NUCL MED BI, 26(4), 1999, pp. 461-466

Abstract

Recently, [Tc-99m]TRODAT-1, the first Tc-99m-labeled tracer for imaging CNS dopamine transporters in humans, was reported. This tracer displayed excellent specific binding to dopamine transporters in the basal ganglia regionof the brain, thus it is potentially useful for the diagnosis of deficit of dopamine transporters in neurodegenerative diseases, such as Parkinson's disease. Preparation of [Tc-99m]TRODAT-1 was previously achieved by a multistep kit formulation. It is highly desirable to further improve the preparation by developing a simplified one-vial formulation with a reduced amount of TRODAT-1 ligand for routine clinical use. To achieve this goal, a seriesof studies to optimize labeling efficiency by varying a combination of factors (amount of free ligand, reaction reagents, and reaction pH) was carried out. [Tc-99m]TRODAT-1 prepared by this new kit formulation was evaluated by assessing the brain uptake and target (striatum) versus nontarget (cerebellum) ratios in rats. Appropriate amounts of various ingredients for a one-vial kit formulation providing greater than or equal to 90% radiolabeling yields were identified. The most consistent and reliable formulation contained 10 mu g of TRODAT-1 (a reduction of free ligand from 200 mu g to 10 mu g), 32 mu g of SnCl2, 10 mg of sodium glucoheptonate, and 840 mu g of disodium EDTA in one vial as a lyophilized kit. It is feasible to reconstitute the vial with [Tc-99m]pertechnetate (0.5-2 mL, less than or equal to 1110 MBq, 30 mCi), resulting in a final solution with a pH value of 4.5-5.0. [Tc-99m]TRODAT-1, prepared by this new kit, was stable at room temperature for 6h. Biodistribution studies of this agent in rats with the new formulation showed similar regional brain distribution as compared with those obtained with the previous preparation (high striatum-to-cerebellum ratio). In conclusion, using this lyophilized one-vial kit formulation, [Tc-99m]TRODAT-1 can be prepared with greater than 90% radiochemical purity. This simplified kit will significantly improve the reliability of preparation of this agent for routine clinical use. NUCL MED BIOL 26;4: 461-4661 1999. (C) 1999 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 07:30:22