Shelton M E, Green M A, Mathias C J, Welch M J, Bergmann S R
Department of Internal Medicine, Washington University School of Medicine, St. Louis, Missouri 63110.
J Nucl Med. 1989 Nov;30(11):1843-7.
Copper(II) pyruvaldehyde bis(N4-methylthiosemicarbazone) ([Cu]PTSM) has shown potential as a flow tracer and can be labeled with the generator-produced positron emitting radionuclide 62Cu as well as with other copper radioisotopes. To define the myocardial handling of [Cu]PTSM, the externally detected single pass extraction and retention of [67Cu]PTSM was characterized after bolus administration in 12 isolated rabbit hearts perfused with erythrocyte-enriched modified Krebs-Henseleit buffer which permitted physiologic flow rates. The myocardial residual (extraction) fraction at control flow rates (approximately 1.5 ml/g/min) was 45 +/- 7(s.d.)% (n = 12), and was invariate with ischemia (flow = 0.15 ml/g/min, n = 4), hyperemia (flow = 3 ml/g/min, n = 4) or with hypoxia induced by perfusion at control flow rates with hypoxic buffer (n = 4) (residual fraction 45 +/- 20, 43 +/- 8, and 49 +/- 8%, respectively, p = N.S.). Once extracted, the tracer was retained with a biologic t1/2 of greater than 3600 min in all groups. The high single-pass extraction, which is not influenced by flow, and the prolonged retention of this tracer under diverse conditions indicate that [Cu]PTSM could be a useful tracer for measuring blood flow with positron emission tomography.
丙酮酸乙醛双(N4 - 甲基硫代半卡巴腙)铜(II)([Cu]PTSM)已显示出作为血流示踪剂的潜力,并且可以用发生器产生的正电子发射放射性核素62Cu以及其他铜放射性同位素进行标记。为了确定[Cu]PTSM在心肌中的摄取情况,在12个用富含红细胞的改良Krebs - Henseleit缓冲液灌注以允许生理流速的离体兔心脏中推注给药后,对[67Cu]PTSM的外部检测单通道提取和滞留进行了表征。在对照流速(约1.5 ml/g/min)下心肌残留(提取)分数为45±7(标准差)%(n = 12),并且在缺血(流速 = 0.15 ml/g/min,n = 4)、充血(流速 = 3 ml/g/min,n = 4)或在对照流速下用缺氧缓冲液灌注诱导的缺氧(n = 4)情况下保持不变(残留分数分别为45±20、43±8和49±8%,p = 无显著性差异)。一旦被提取,示踪剂在所有组中的生物学半衰期大于3600分钟。这种示踪剂的高单通道提取不受流速影响,并且在不同条件下的长时间滞留表明[Cu]PTSM可能是一种用于正电子发射断层扫描测量血流的有用示踪剂。