[3H]哇巴因在体外与脑和心脏组织的可饱和的、不依赖三磷酸腺苷的结合
Saturable adenosine 5'-triphosphate-independent binding of [3H]-ouabain to brain and cardiac tissue in vitro.
作者信息
Akera T, Brody T M, Wiest S A
出版信息
Br J Pharmacol. 1979 Mar;65(3):403-9. doi: 10.1111/j.1476-5381.1979.tb07844.x.
Abstract
- Several investigators have proposed that membrane Na+, K+-adenosine 5'-triphosphatase (Na+, K+-ATPase) is a mechanism for the transmembrane transport of cardiac glycosides, rather than the receptor for pharmacological actions of these agents. This implies that the glycosides bind to an intracellular constituent (receptor) other than Na+, K+-ATPase. 2. In search for such a receptor site, saturable ATP-independent [3H]-ouabain binding was studied in rat brain and dog and guinea-pig heart homogenates. The binding of the glucoside to this site results in a relatively unstable complex which is stabilized by K+ to a lesser extent than is the complex formed with the ATP-dependent binding to Na+, K+-ATPase. 3. The ATP-independent ouabain binding sites are more abundant in rat brain tissue than in cardiac tissue, and have a lower ouabain affinity compared to the binding sites on Na+, K+-ATPase. 4. These results do not support the contention that there are intracellular inotropic receptors for digitalis.
摘要
- 几位研究者提出，膜钠钾-腺苷三磷酸酶（Na⁺，K⁺-ATP酶）是强心苷跨膜转运的一种机制，而非这些药物药理作用的受体。这意味着苷类与Na⁺，K⁺-ATP酶以外的细胞内成分（受体）结合。2. 为寻找这样一个受体位点，在大鼠脑、犬和豚鼠心脏匀浆中研究了可饱和的非ATP依赖性[³H]哇巴因结合。糖苷与该位点的结合形成相对不稳定的复合物，与依赖ATP结合到Na⁺，K⁺-ATP酶形成的复合物相比，钾对其稳定作用较小。3. 非ATP依赖性哇巴因结合位点在大鼠脑组织中比在心脏组织中更丰富，且与Na⁺，K⁺-ATP酶上的结合位点相比，其对哇巴因的亲和力更低。4. 这些结果不支持存在洋地黄细胞内变力性受体这一论点。
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