68GaTHM2BED: a potential generator-produced tracer of myocardial perfusion for positron emission tomography

Susan L Madsen , Michael J Welch , Ramunas J Motekaitis , Arthur E Martell
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引用次数: 7

Abstract

THM2BED [N,N,N′,N′-tetrakis-(2-hydroxy-3,5-dimethylbenzyl)ethylenediamine] is a new hexadentate ligand which has been synthesized and complexed with gallium isotopes. A conditional stability constant of 22.3 and a pM value of 20.7 have been determined for GaTHM2BED at physiological pH. Hexachelated and pentachelated complexes of GaTHM2BED have been isolated via preparatory HPLC and evaluated individually. The hexachelated isomer of 68GaTHM2BED clears slowly from the myocardium of rats and at 1 h post-injection the heart-to-blood ratio is 1.65. The data ratio indicates that this radiotracer may be capable of measuring blood flow in the heart. The ability of 68GaTHM2BED to delineate myocardial tissue in a dog has been evaluated and good images were obtained using hexachelated 68GaTHM2BED. There is evidence that this complex penetrates the blood-brain barrier.

68GaTHM2BED:一种潜在的心肌灌注示踪剂,用于正电子发射断层扫描
THM2BED [N,N,N ',N ' -四基-(2-羟基-3,5-二甲基苄基)乙二胺]是一种新的六齿配体,已合成并与镓同位素络合。经测定,GaTHM2BED在生理ph值下的条件稳定常数为22.3,pM值为20.7。通过预备HPLC分离出GaTHM2BED的六价和五价配合物,并分别进行了评价。68GaTHM2BED的六化异构体从大鼠心肌中缓慢清除,注射后1 h心血比为1.65。数据比率表明,这种放射性示踪剂可能能够测量心脏的血流。68GaTHM2BED对狗心肌组织的描画能力进行了评估,使用hexachelated 68GaTHM2BED获得了良好的图像。有证据表明这种复合物能穿透血脑屏障。
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