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新型抗心绞痛药物2-烟酰胺基乙基硝酸盐(SG-75)对环磷酸腺苷磷酸二酯酶活性的影响。

Effects of 2-nicotinamidethyl nitrate (SG-75), a new antianginal drug, on the cyclic AMP phosphodiesterase activity.

作者信息

Endoh M, Yanagisawa T, Taira N

出版信息

Tohoku J Exp Med. 1980 Feb;130(2):199-201. doi: 10.1620/tjem.130.199.

DOI:10.1620/tjem.130.199
PMID:6247783
Abstract

The effect of a potent coronary vasodilator, SG-75, on the purified cyclic AMP phosphodiesterase of the bovine heart was compared with that of papaverine. SG-75 inhibited the phosphodiesterase activity in a competitive manner, the IC50 being 10 mM. SG-75 was approximately 300 times less potent than papaverine in inhibiting the phosphodiesterase activity. Thus, it is unlikely that the phosphodiesterase inhibition by SG-75 is involved in its vasodilator action.

摘要

将一种强效冠状动脉血管扩张剂SG - 75对牛心脏纯化环磷酸腺苷磷酸二酯酶的作用与罂粟碱进行了比较。SG - 75以竞争性方式抑制磷酸二酯酶活性,半数抑制浓度(IC50)为10 mM。在抑制磷酸二酯酶活性方面,SG - 75的效力约为罂粟碱的300分之一。因此,SG - 75对磷酸二酯酶的抑制作用不太可能涉及其血管扩张作用。

相似文献

1
Effects of 2-nicotinamidethyl nitrate (SG-75), a new antianginal drug, on the cyclic AMP phosphodiesterase activity.新型抗心绞痛药物2-烟酰胺基乙基硝酸盐(SG-75)对环磷酸腺苷磷酸二酯酶活性的影响。
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Inhibition of cyclic AMP phosphodiesterase by 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methylamino)] ethyl ester 5-methyl ester hydrochloride (YC-93), a potent vasodilator.强效血管扩张剂2,6 - 二甲基 - 4 - (3 - 硝基苯基) - 1,4 - 二氢吡啶 - 3,5 - 二羧酸3 - [2 - (N - 苄基 - N - 甲基氨基)]乙酯5 - 甲酯盐酸盐(YC - 93)对环磷酸腺苷磷酸二酯酶的抑制作用
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Effects of 2-nicotinamidethyl nitrate (SG-75) and/or nitroglycerin on systemic hemodynamics and coronary blood flow in conscious dogs.2-烟酰胺乙基硝酸盐(SG-75)和/或硝酸甘油对清醒犬全身血流动力学和冠状动脉血流量的影响。
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Effect of 2-nicotinamidethyl nitrate (SG-75) on membrane potentials of canine Purkinje fibers.2-硝酸烟酰胺乙酯(SG-75)对犬浦肯野纤维膜电位的影响。
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引用本文的文献

1
Electrophysiologic effects of nicorandil, a new antianginal agent, on action potentials and membrane currents of rabbit atrioventricular node.新型抗心绞痛药物尼可地尔对兔房室结动作电位和膜电流的电生理效应
Naunyn Schmiedebergs Arch Pharmacol. 1987 May;335(5):567-74. doi: 10.1007/BF00169126.
2
Nicorandil increases coronary blood flow predominantly by K-channel opening mechanism.尼可地尔主要通过开放钾通道机制增加冠状动脉血流量。
Cardiovasc Drugs Ther. 1990 Aug;4(4):1119-26. doi: 10.1007/BF01856508.
3
Pharmacology and therapeutic effects of nicorandil.
尼可地尔的药理学与治疗作用。
Cardiovasc Drugs Ther. 1990 Aug;4(4):1075-88. doi: 10.1007/BF01856503.
4
Specific but differential antagonism by glibenclamide of the vasodepressor effects of cromakalim and nicorandil in spinally-anaesthetized dogs.格列本脲对脊髓麻醉犬克罗卡林和尼可地尔血管降压作用的特异性但有差异的拮抗作用。
Br J Pharmacol. 1990 Jul;100(3):413-6. doi: 10.1111/j.1476-5381.1990.tb15820.x.