Hagane K, Akera T, Stemmer P, Yao A Z, Yokoyama C
Department of Pharmacology and Toxicology, Michigan State University, East Lansing 48824.
Eur J Pharmacol. 1988 Jan 27;146(1):137-44. doi: 10.1016/0014-2999(88)90495-5.
In intact heart muscle cells incubated in a physiological solution, i.e. under the condition in which the cardiac glycosides produce pharmacological and toxicological effects, receptors for these actions of the glycosides should be available to ouabain. In cell homogenates, [3H]ouabain binding observed in the presence of Mg2+ and inorganic phosphate represents binding of the glycoside to Na+, K+-ATPase. Therefore, numbers of these two types of [3H]ouabain binding sites were compared using viable myocyte preparations obtained from ventricular muscle of guinea-pig heart. The number of ouabain binding sites observed in viable myocytes in the absence of Ca2+ and K+ was not different from the number of ouabain binding sites on Na+, K+-ATPase observed with sodium dodecylsulfate-treated homogenates prepared from isolated myocytes. These results do not support the hypothesis that there are receptors for the pharmacological or toxic actions of ouabain other than those that are associated with sarcolemmal Na+, K+-ATPase.
在生理溶液中孵育的完整心肌细胞中,即在强心苷产生药理和毒理作用的条件下,这些苷类作用的受体应该对哇巴因可用。在细胞匀浆中,在Mg2+和无机磷酸盐存在下观察到的[3H]哇巴因结合代表苷类与Na+,K+-ATP酶的结合。因此,使用从豚鼠心脏心室肌获得的活心肌细胞制剂比较了这两种类型的[3H]哇巴因结合位点的数量。在不存在Ca2+和K+的情况下,在活心肌细胞中观察到的哇巴因结合位点数量与用从分离的心肌细胞制备的十二烷基硫酸钠处理的匀浆观察到的Na+,K+-ATP酶上的哇巴因结合位点数量没有差异。这些结果不支持除了与肌膜Na+,K+-ATP酶相关的受体之外,存在哇巴因药理或毒性作用受体的假设。