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地高辛和SC4453对从人心脏、豚鼠心脏和豚鼠大脑制备的(钠+钾)-ATP酶的抑制作用。

Inhibition by digoxin and SC4453 of (Na+ + K+)-ATPase prepared from human heart, guinea-pig heart and guinea-pig brain.

作者信息

Godfraind T, Tona Lutete D N

出版信息

Eur J Pharmacol. 1979 Dec 20;60(4):329-36. doi: 10.1016/0014-2999(79)90237-1.

DOI:10.1016/0014-2999(79)90237-1
PMID:230981
Abstract

SC4453 is a digoxin analogue with a pyridazine instead of a lactone ring on C17 beta. SC4453 was compared with digoxin with respect to inhibition of (Na+ + K+)-ATPase prepared from human heart, guinea-pig heart and guinea-pig brain. SC4453 was slightly less potent than digoxin but showed a similar sensitivity to K+. As for cardenolides, species differences in sensitivity to SC4453 were accounted for by differences in the rate of dissociation from the receptors. These observations confirm that the human heart is one of the tissues most sensitive to cardiac glycosides.

摘要

SC4453是一种地高辛类似物,其C17β位上是哒嗪环而非内酯环。将SC4453与地高辛在抑制从人心脏、豚鼠心脏和豚鼠大脑制备的(钠+钾)-ATP酶方面进行了比较。SC4453的效力略低于地高辛,但对钾的敏感性相似。至于强心苷,对SC4453敏感性的物种差异是由从受体解离速率的差异造成的。这些观察结果证实,人心脏是对强心苷最敏感的组织之一。

相似文献

1
Inhibition by digoxin and SC4453 of (Na+ + K+)-ATPase prepared from human heart, guinea-pig heart and guinea-pig brain.地高辛和SC4453对从人心脏、豚鼠心脏和豚鼠大脑制备的(钠+钾)-ATP酶的抑制作用。
Eur J Pharmacol. 1979 Dec 20;60(4):329-36. doi: 10.1016/0014-2999(79)90237-1.
2
Interaction of digoxin and SC4453 with the (Na+ + K+)-ATPase from guinea-pig heart and brain.地高辛和SC4453与豚鼠心脏和大脑的(钠+钾)-ATP酶的相互作用。
Arch Int Pharmacodyn Ther. 1979 May;239(1):171-2.
3
The cardioactive properties of SC4453, a digoxin analogue with a C17 beta-pyridazine ring.
Eur J Pharmacol. 1979 Dec 20;60(4):337-44. doi: 10.1016/0014-2999(79)90238-3.
4
Cross-resistance and biochemical studies with two classes of HeLa cell mutants resistant to cardiac glycosides. The unusual behavior of cardenolide SC4453.对两类耐强心苷的海拉细胞突变体进行的交叉抗性和生化研究。强心甾SC4453的异常行为。
J Biol Chem. 1985 Jun 10;260(11):6843-50.
5
Effects of K+ on the interaction between cardiac glycosides and Na,K-ATPase.钾离子对强心苷与钠钾ATP酶相互作用的影响。
Eur J Pharmacol. 1985 May 8;111(2):147-57. doi: 10.1016/0014-2999(85)90751-4.
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Biochemical and cross-resistance studies with HeLa cell mutants resistant to cardiac glycoside SC4453. Regulation of the resistant form of Na+/K+-ATPase in the mutant cells.对耐强心苷SC4453的HeLa细胞突变体进行的生化及交叉耐药性研究。突变体细胞中耐Na+/K+-ATP酶形式的调控。
J Biol Chem. 1986 Feb 15;261(5):2034-40.
7
Influence of 16 beta formylation on Na, K-ATPase inhibition by cardiac glycosides.16β-甲酰化对强心苷抑制钠钾ATP酶的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Nov;321(2):135-9. doi: 10.1007/BF00518481.
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[Characterization of an endogenous factor with digitalis-like activity in the heart of the guinea pig (I): Inhibition of Na,K-ATPase)].
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Sensitivity to cardiac glycosides of (Na + K) ATPase prepared from human heart, guinea-pig heart and guinea-pig brain.
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Origin of differences of inhibitory potency of cardiac glycosides in Na+/K+-transporting ATPase from human cardiac muscle, human brain cortex and guinea-pig cardiac muscle.
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Basic Res Cardiol. 1983 Nov-Dec;78(6):695-705. doi: 10.1007/BF01907217.
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Influence of 16 beta formylation on Na, K-ATPase inhibition by cardiac glycosides.16β-甲酰化对强心苷抑制钠钾ATP酶的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Nov;321(2):135-9. doi: 10.1007/BF00518481.
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The lead structure in cardiac glycosides is 5 beta, 14 beta-androstane-3 beta 14-diol.强心苷类的先导结构是5β,14β-雄甾烷-3β,14-二醇。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jun;329(4):414-26. doi: 10.1007/BF00496377.
6
Distribution of SC-4453, a new semi-synthetic derivative of digoxin, following an infusion preceded by an i.v. loading dose in the guinea-pig. Binding to plasma proteins.在豚鼠静脉注射负荷剂量后进行输注后,地高辛新的半合成衍生物SC - 4453的分布。与血浆蛋白的结合。
Eur J Drug Metab Pharmacokinet. 1988 Jan-Mar;13(1):19-22. doi: 10.1007/BF03189923.