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The cardioactive properties of SC4453, a digoxin analogue with a C17 beta-pyridazine ring.

作者信息

Godfraind T, Ghysel-Burton J

出版信息

Eur J Pharmacol. 1979 Dec 20;60(4):337-44. doi: 10.1016/0014-2999(79)90238-3.

DOI:10.1016/0014-2999(79)90238-3
PMID:527669
Abstract

SC4453 is a digoxin analogue with a pyridazine instead of a lactone ring in C17 beta. SC4453 was compared with digoxin with respect to effect on contractility and on activity of the sodium pump in guinea-pig isolated left atria stimulated at 3.3 Hz. The two glycosides stimulated the sodium pump at low concentrations and inhibited at high concentrations. At the time to peak inotropic effect, for a similar inhibition of the Na pump, the increase in systolic tension was higher with SC4453 than with digoxin, whereas the increase in diastolic tension was similar for both. These observations confirm that the inhibition of the Na pump is not the only mechanism responsible for the positive inotropic effect of cardiac glycosides.

摘要

相似文献

1
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.
2
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.
3
Stimulation and inhibition of the sodium pump by cardioactive steroids in relation to their binding sites and their inotropic effect on guinea-pig isolated atria.强心甾体对钠泵的刺激与抑制作用及其与结合位点的关系以及对豚鼠离体心房的变力效应
Br J Pharmacol. 1979 Jun;66(2):175-84. doi: 10.1111/j.1476-5381.1979.tb13662.x.
4
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.
5
The action of digoxin and digoxigenin-monodigitoxoside on the sodium pump and on the contractility in isolated guinea-pig atria.地高辛和洋地黄毒苷-单洋地黄毒糖苷对豚鼠离体心房钠泵及收缩性的作用。
Arch Int Pharmacodyn Ther. 1978 Aug;234(2):340-1.
6
Inotropic action and myocardial uptake of digoxin and betamethyldigoxin in isolated guinea pig atria.地高辛和倍他甲基地高辛在离体豚鼠心房中的变力作用及心肌摄取
Acta Pharmacol Toxicol (Copenh). 1977 May;40(5):545-52.
7
Positive inotropic action of digoxigenin and sodium pump inhibition: effects of enhanced sodium influx.洋地黄毒苷的正性肌力作用与钠泵抑制:钠内流增加的影响
J Pharmacol Exp Ther. 1980 Apr;213(1):105-9.
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Differential effect of potassium on the action of digoxin and digoxigenin in guinea-pig heart.钾对豚鼠心脏中地高辛和洋地黄毒苷作用的差异效应。
Eur J Pharmacol. 1979 Aug 15;57(4):343-51. doi: 10.1016/0014-2999(79)90497-7.
9
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。
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Effects of quinidine on the cardiac-glycoside sensitivity of guinea-pig and rat heart.奎尼丁对豚鼠和大鼠心脏洋地黄苷敏感性的影响。
J Pharmacol Exp Ther. 1981 Jun;217(3):559-65.

引用本文的文献

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Ouabain effects on intracellular potassium activity and contractile force in cat papillary muscle.哇巴因对猫乳头肌细胞内钾活性和收缩力的影响。
J Clin Invest. 1981 Oct;68(4):942-56. doi: 10.1172/jci110349.
2
Proceedings of the British Pharmacological Society. 10th-12th September, 1980. Abstracts.英国药理学会会议记录。1980年9月10日至12日。摘要。
Br J Pharmacol. 1981 Mar;72(3):487P-590P. doi: 10.1111/j.1476-5381.1981.tb11001.x.
3
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.