Takeo S, Taam G M, Beamish R E, Dhalla N S
J Pharmacol Exp Ther. 1980 Sep;214(3):688-93.
The influence of adrenochrome (1-100 microgram/ml or 5.6 x 10(-6)-5.4 x 10(-4) M) on microsomal calcium binding, calcium uptake and Ca++-stimulated Mg++-dependent adenosine triphosphatase (ATPase) activities was studied in vitro. Adrenochrome decreased microsomal calcium binding, calcium uptake and Ca++-stimulated Mg++-dependent ATPase activities. The inhibitory effect of adrenochrome on microsomal calcium uptake activity of the isolated membrane was independent of pH (6.0-8.0), calcium concentrations (10-200 muM), protein concentration (0.02-0.10 mg/ml), temperature (25-37 degrees C) and incubation time (2-30 min). Kinetic study of calcium uptake activity in different concentrations of ATP showed that the inhibition was of a mixed type. Perfusion of hearts with adrenochrome resulted in marked depression in contractile force and the microsomal fraction obtained from these hearts showed depressed calcium binding, calcium uptake and Ca++-stimulated Mg++-dependent ATPase activities. The depression in microsomal The influence of adrenochrome (1-100 microgram/ml or 5.6 x 10(-6)-an irreversible nature. It is proposed that cardiodepressant action of adrenochrome may partly be explained on the basis of its inhibitory effect on the calcium transporting ability of the sarcoplasmic reticulum.
在体外研究了肾上腺色素(1 - 100微克/毫升或5.6×10⁻⁶ - 5.4×10⁻⁴摩尔)对微粒体钙结合、钙摄取以及Ca²⁺刺激的Mg²⁺依赖性腺苷三磷酸酶(ATP酶)活性的影响。肾上腺色素降低了微粒体钙结合、钙摄取以及Ca²⁺刺激的Mg²⁺依赖性ATP酶活性。肾上腺色素对分离膜微粒体钙摄取活性的抑制作用与pH(6.0 - 8.0)、钙浓度(10 - 200微摩尔)、蛋白质浓度(0.02 - 0.10毫克/毫升)、温度(25 - 37摄氏度)和孵育时间(2 - 30分钟)无关。对不同ATP浓度下钙摄取活性的动力学研究表明,这种抑制是混合型的。用肾上腺色素灌注心脏导致收缩力明显降低,从这些心脏获得的微粒体部分显示钙结合、钙摄取以及Ca²⁺刺激的Mg²⁺依赖性ATP酶活性降低。微粒体中的这种降低具有不可逆性。有人提出,肾上腺色素的心脏抑制作用可能部分基于其对肌浆网钙转运能力的抑制作用来解释。