McCall D, Zimmer L J, Katz A M
Circ Res. 1985 Mar;56(3):370-6. doi: 10.1161/01.res.56.3.370.
The kinetics of thallium exchange in cultured rat myocardial cells were studied and compared to those of potassium in the same tissue. Studies were carried out using low concentrations (10 nM to 5 microM) of thallium-204, approximating those likely to be encountered during clinical myocardial scintigraphy. Both thallium uptake and release could be described by a single exponential with a half-time of exchange which was approximately half that of potassium and which was largely independent of extracellular thallium concentration. Some 60% of thallium uptake occurred via an "active" or ouabain-inhibitable mechanism which, in the absence of extracellular potassium, could be activated by low concentrations (10 nM to 5 microM) of thallium. The apparent Km for thallium on this active transport mechanism was 2-7 microM. Increasing extracellular potassium from 0-10 mM caused significant, concentration-dependent decreases in both the total and the active component of the thallium influx. Similarly nonradioactive thallium (0.10 microM to 0.10 mM) caused a concentration-dependent decrease in active potassium influx. Analysis of these results by both Lineweaver-Burk plots and Dixon plots confirmed competitive inhibition, potassium on thallium influx and vice versa, for the active component of the fluxes, and noncompetitive in the remainder. These findings indicate that active transport accounts for the greater portion of the influx of thallium and potassium, and that this active transport occurs via a common mechanism.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了培养的大鼠心肌细胞中铊交换的动力学,并将其与同一组织中钾的动力学进行了比较。使用低浓度(10 nM至5 microM)的铊-204进行研究,该浓度接近临床心肌闪烁显像时可能遇到的浓度。铊的摄取和释放都可以用单一指数来描述,其交换半衰期约为钾的一半,并且在很大程度上与细胞外铊浓度无关。约60%的铊摄取是通过一种“主动”或哇巴因可抑制的机制发生的,在没有细胞外钾的情况下,低浓度(10 nM至5 microM)的铊可以激活该机制。铊在这种主动转运机制上的表观Km为2 - 7 microM。将细胞外钾浓度从0增加到10 mM会导致铊流入的总量和主动成分都显著降低,且呈浓度依赖性。同样,非放射性铊(0.10 microM至0.10 mM)会导致主动钾流入呈浓度依赖性降低。通过Lineweaver - Burk图和Dixon图对这些结果进行分析,证实了对于通量的主动成分,钾对铊流入存在竞争性抑制,反之亦然,而在其余部分则为非竞争性抑制。这些发现表明,主动转运占铊和钾流入的较大部分,并且这种主动转运通过一种共同机制发生。(摘要截短至250字)