Comparison of neutral and cationic myocardial perfusion agents: Characteristics of accumulation in cultured cells

James F. Kronauge , Mary L. Chiu , Jeffrey S. Cone , Alan Davison , B.Leonard Holman , Alun G. Jones , David Piwnica-Worms
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引用次数: 35

Abstract

Uptake and washout kinetics of two new neutral lipophilic technetium-99m-labeled boronic acid adducts of technetium tris(dioxime) (BATO complexes) were studied in monolayers of contractile chick heart cells and compared to the cationic myocardial perfusion agents, 99mTc(CNCH2C(CH3)2OCH3)+6 (Tc-MIBI) and 201Tl+. 99mTcCl(CDOH)2(CDO)(BCH3), where CDO = cyclohexanedione dioxime (CDO-MeB), had a 7-fold greater net accumulation than Tc-MIBI and the most rapid unidirectional washout with a fast initial phase and a slower secondary component. Incubation with cationic membrane transport inhibitors or metabolic inhibitors had little or modest influence, respectively, on uptake of these BATO complexes. Studies with NIH 3T3 fibroblasts indicated that the neutral complexes did not show myocyte specific accumulation.

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中性和阳离子心肌灌注剂的比较:培养细胞的蓄积特征
本文研究了两种新的中性亲脂性锝-99m标记的硼酸加合物(BATO复合物)在收缩性鸡心脏细胞单层内的摄取和清除动力学,并与阳离子心肌灌注剂99mTc(CNCH2C(CH3)2OCH3)+6 (Tc-MIBI)和201Tl+进行了比较。99mTcCl(CDOH)2(CDO)(BCH3) (CDO =环己二酮二肟(CDO- meb))的净积累量是Tc-MIBI的7倍,单向冲蚀速度最快,初始阶段快,次级组分慢。与阳离子膜转运抑制剂或代谢抑制剂孵育分别对这些BATO复合物的摄取影响很小或适度。对NIH 3T3成纤维细胞的研究表明,中性复合物没有表现出肌细胞特异性积累。
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