双嘧达莫：一种强效的前列环素（PGI2）生物合成刺激剂。
Dipyridamole: a potent stimulator of prostacyclin (PGI2) biosynthesis.
作者信息
Blass K E, Block H U, Förster W, Pönicke K
出版信息
Br J Pharmacol. 1980 Jan;68(1):71-3. doi: 10.1111/j.1476-5381.1980.tb10700.x.
Abstract
1 Dipyridamole (0.01 to 0.75 mM) increased prostacyclin (PGI2) biosynthesis from tritiated arachidonic acid in rat stomach fundus homogenates by 21 to 350%. The transformation of prostaglandin H2 (PGH2) to PGI2 by a microsomal fraction of pig aorta was stimulated by dipyridamole at 0.1 M by 63%. 2 In the isolated perfused heart of the rabbit dipyridamole at 1 and 5 micrograms/ml increased PGI2 release by 70% and 146% respectively. 3 Our results show a stimulation of the second step in PGI2 biosynthesis (from endoperoxides) by dipyridamole. This effect should be considered in relation to the therapeutic usage of the drug in myocardial infarction.
摘要
- 双嘧达莫（0.01至0.75毫摩尔）使大鼠胃底匀浆中由氚标记的花生四烯酸合成前列环素（PGI2）的量增加了21%至350%。双嘧达莫在0.1摩尔浓度时可使猪主动脉微粒体部分将前列腺素H2（PGH2）转化为PGI2的过程增强63%。2. 在离体灌注的兔心脏中，1微克/毫升和5微克/毫升的双嘧达莫分别使PGI2释放增加70%和146%。3. 我们的结果表明双嘧达莫可刺激PGI2生物合成的第二步（从内过氧化物开始）。在考虑该药物在心肌梗死治疗中的应用时应顾及这一效应。
相似文献
1
Dipyridamole: a potent stimulator of prostacyclin (PGI2) biosynthesis.双嘧达莫：一种强效的前列环素（PGI2）生物合成刺激剂。
Br J Pharmacol. 1980 Jan;68(1):71-3. doi: 10.1111/j.1476-5381.1980.tb10700.x.
2
Transformation of arachidonic acid and prostaglandin endoperoxides by the guinea pig heart. Formation of RCS and prostacyclin.豚鼠心脏对花生四烯酸和前列腺素内过氧化物的转化。RCS和前列环素的形成。
Eur J Pharmacol. 1978 Jan 1;47(1):103-14. doi: 10.1016/0014-2999(78)90380-1.
3
Myocardial biosynthesis of prostaglandins with special consideration of prostacyclin and the influence of dipyridamole and propranolol.
Adv Myocardiol. 1983;4:531-7. doi: 10.1007/978-1-4757-4441-5_51.
4
5
In vivo injection of dipyridamole stimulates the synthesis of prostacyclin-like substances in human varicose veins.
Biomed Biochim Acta. 1984;43(3):K6-8.
6
[Stimulation of prostacyclin biosynthesis as a possible mechanism of action of dipyridamole (author's transl)].
Arzneimittelforschung. 1981;31(12):2075-82.
7
Significance of myocardial prostaglandin biosynthesis and the influence of mechanical loading, endogenous mediators and cardiovascular drugs.
Biomed Biochim Acta. 1984;43(8-9):S147-50.
8
Enhanced prostacyclin production by dipyridamole in man.双嘧达莫在人体内增强前列环素的生成。
Eur J Clin Pharmacol. 1981;21(1):9-15. doi: 10.1007/BF00609581.
9
Conversions of prostaglandin endoperoxides by prostacyclin synthase from pig aorta.猪主动脉前列环素合酶对前列腺素内过氧化物的转化作用。
Prostaglandins. 1980 Jun;19(6):969-76. doi: 10.1016/0090-6980(80)90129-x.
10
Effect of dipyridamole on prostaglandin generation by human platelets and vessel walls.双嘧达莫对人血小板和血管壁生成前列腺素的影响。
Prostaglandins. 1982 Dec;24(6):751-61. doi: 10.1016/0090-6980(82)90056-9.
引用本文的文献
1
Dipyridamole decreases dialysis risk and improves survival in patients with pre-dialysis advanced chronic kidney disease.双嘧达莫可降低透析前晚期慢性肾病患者的透析风险并提高生存率。
Oncotarget. 2017 Aug 3;9(4):5368-5377. doi: 10.18632/oncotarget.19850. eCollection 2018 Jan 12.
2
Additive effects of statin and dipyridamole on cerebral blood flow and stroke protection.他汀类药物和双嘧达莫对脑血流量及中风保护的相加作用。
J Cereb Blood Flow Metab. 2008 Jul;28(7):1285-93. doi: 10.1038/jcbfm.2008.24. Epub 2008 Apr 2.
3
Translational therapeutics of dipyridamole.双嘧达莫的转化治疗学
Arterioscler Thromb Vasc Biol. 2008 Mar;28(3):s39-42. doi: 10.1161/ATVBAHA.107.160226. Epub 2008 Jan 3.
4
Novel C2-purine position analogs of nitrobenzylmercaptopurine riboside as human equilibrative nucleoside transporter 1 inhibitors.新型硝基苄基巯基嘌呤核糖核苷的C2-嘌呤位置类似物作为人平衡核苷转运体1抑制剂
Bioorg Med Chem. 2007 Dec 15;15(24):7726-37. doi: 10.1016/j.bmc.2007.08.058. Epub 2007 Sep 1.
5
Adenosine transporter antagonism in humans augments vasodilator responsiveness to adenosine, but not exercise, in both adenosine responders and non-responders.在人体中，腺苷转运体拮抗作用可增强腺苷反应者和非反应者对腺苷的血管舒张反应性，但对运动引起的血管舒张反应性无增强作用。
J Physiol. 2007 Feb 15;579(Pt 1):237-45. doi: 10.1113/jphysiol.2006.123000. Epub 2006 Dec 7.
6
The antiarrhythmic effects of the nucleoside transporter inhibitor, R75231, in anaesthetized pigs.核苷转运体抑制剂R75231对麻醉猪的抗心律失常作用。
Br J Pharmacol. 1993 Jun;109(2):592-9. doi: 10.1111/j.1476-5381.1993.tb13612.x.
7
Studies of the nucleoside transporter inhibitor, draflazine, in the human myocardium.核苷转运体抑制剂draflazine在人体心肌中的研究。
Br J Pharmacol. 1994 May;112(1):137-42. doi: 10.1111/j.1476-5381.1994.tb13043.x.
8
Purine metabolism in the heart. Strategies for protection against myocardial ischaemia.心脏中的嘌呤代谢。预防心肌缺血的策略。
Pharm World Sci. 1994 Apr 15;16(2):69-76. doi: 10.1007/BF01880658.
9
Hemodynamic and neurohumoral effects of various grades of selective adenosine transport inhibition in humans. Implications for its future role in cardioprotection.不同程度的选择性腺苷转运抑制对人体的血流动力学和神经体液影响。及其在心脏保护中未来作用的意义。
J Clin Invest. 1995 Feb;95(2):658-68. doi: 10.1172/JCI117711.
10
Chemical sympathectomy abolishes the increase in blood pressure of linoleic acid deficient fed rats induced by salt loading.
Naunyn Schmiedebergs Arch Pharmacol. 1981 Aug;317(1):78-80. doi: 10.1007/BF00506261.
本文引用的文献
1
[COMPETITIVE INHIBITION OF CATALYZED ADENOSINE DIFFUSION AS THE MECHANISM OF THE CORONARY DILATING EFFECT OF A PYRIMIDO-PYRIMIDINE DERIVATIVE].[嘧啶-嘧啶衍生物冠状动脉扩张作用机制为催化腺苷扩散的竞争性抑制]
Pflugers Arch Gesamte Physiol Menschen Tiere. 1964 Jul 1;280:141-57.
2
3
Arterial walls are protected against deposition of platelet thrombi by a substance (prostaglandin X) which they make from prostaglandin endoperoxides.动脉壁可通过一种由前列腺素内过氧化物生成的物质（前列腺素X）来防止血小板血栓的沉积。
Prostaglandins. 1976 Nov;12(5):685-713. doi: 10.1016/0090-6980(76)90047-2.
4
An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation.从动脉中分离出的一种酶可将前列腺素内过氧化物转化为一种抑制血小板聚集的不稳定物质。
Nature. 1976 Oct 21;263(5579):663-5. doi: 10.1038/263663a0.
5
Prostacyclin: a potentially valuable agent for preserving myocardial tissue in acute myocardial ischemia.
Science. 1978 Apr 7;200(4337):52-4. doi: 10.1126/science.345441.
6
Prostacyclin is the major prostaglandin released from the isolated perfused rabbit and rat heart.前列环素是从离体灌注的兔和大鼠心脏释放的主要前列腺素。
Nature. 1977 Jul 14;268(5616):160-3. doi: 10.1038/268160a0.
Zotero 插件