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13,14-脱氢前列环素甲酯的冠状动脉舒张活性:与前列环素及其他前列腺素的比较。

Coronary vasodilator activity of 13,14-dehydroprostacyclin methyl ester: comparison with prostacyclin and other prostanoids.

作者信息

Hyman A L, Kadowitz P J, Lands W E, Crawford C G, Fried J, Barton J

出版信息

Proc Natl Acad Sci U S A. 1978 Jul;75(7):3522-6. doi: 10.1073/pnas.75.7.3522.

DOI:10.1073/pnas.75.7.3522
PMID:356056
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC392810/
Abstract

The effects of a recently synthesized, stable prostacyclin (PGI2) analog, 13,14-dehydro-PGI2 methyl ester, and authentic PGI2 and several other prostanoids on the coronary circulation were investigated in the intact dog by using a new technique to measure coronary sinus blood flow. The PGI2 analog, PGI2, and prostaglandin (PG) E2 and D2 each increased coronary sinus blood flow in a dose-related fashion when injected into the left coronary artery. The analog and PGE2 had similar vasodilator activity while PGI2 was slightly more potent. PGD2 was a moderately active coronary vasodilator whereas PGF2alpha was inactive. The coronary vasodilator effects of PGI2, its analog, PGE2, and PGD2 occurred at doses that had little effect on aortic pressure, left ventricular pressure and its first derivative, or on cardiac output and heart rate. The prostaglandin precursor arachidonic acid and the endoperoxide intermediate PGH2 both increased coronary sinus blood flow in a dose-dependent manner. The effects of arachidonic acid were inhibited by indomethacin. These data show that PGE2, PGI2, and a stable PGI2 analog are potent vasodilators in the canine coronary vascular bed and suggest that the vasodilator effects of arachidonic acid and PGH2 may be due to the formation of PGE2, PGD2, or PGI2 in the dog heart.

摘要

利用一种测量冠状窦血流量的新技术,在完整的犬身上研究了一种新合成的稳定前列环素(PGI2)类似物13,14-脱氢-PGI2甲酯、天然PGI2以及其他几种前列腺素对冠脉循环的影响。当将PGI2类似物、PGI2、前列腺素(PG)E2和D2注入左冠状动脉时,它们均以剂量相关的方式增加冠状窦血流量。该类似物和PGE2具有相似的血管舒张活性,而PGI2的活性稍强。PGD2是一种中度活性的冠脉血管舒张剂,而PGF2α无活性。PGI2及其类似物、PGE2和PGD2的冠脉血管舒张作用发生时的剂量,对主动脉压、左心室压力及其一阶导数、心输出量和心率几乎没有影响。前列腺素前体花生四烯酸和内过氧化物中间体PGH2均以剂量依赖的方式增加冠状窦血流量。花生四烯酸的作用被吲哚美辛抑制。这些数据表明,PGE2、PGI2和一种稳定的PGI2类似物是犬冠脉血管床中的强效血管舒张剂,并提示花生四烯酸和PGH2的血管舒张作用可能是由于犬心脏中形成了PGE2、PGD2或PGI2。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e2ae/392810/555088b39fd4/pnas00019-0519-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e2ae/392810/555088b39fd4/pnas00019-0519-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e2ae/392810/555088b39fd4/pnas00019-0519-a.jpg

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Coronary vasodilator activity of 13,14-dehydroprostacyclin methyl ester: comparison with prostacyclin and other prostanoids.13,14-脱氢前列环素甲酯的冠状动脉舒张活性:与前列环素及其他前列腺素的比较。
Proc Natl Acad Sci U S A. 1978 Jul;75(7):3522-6. doi: 10.1073/pnas.75.7.3522.
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引用本文的文献

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Basic Res Cardiol. 1981 May-Jun;76(3):313-27. doi: 10.1007/BF01907775.
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Prostaglandins evoke a whole variety of responses in the lung.前列腺素可在肺部引发各种各样的反应。
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Coronary vasoconstrictor and vasodilator actions of arachidonic acid in the isolated perfused heart of the rat.

本文引用的文献

1
Polyhydroxy cyclic ethers formed from tritiated arachidonic acid by acetone powders of sheep seminal vesicles.由氚标记的花生四烯酸通过绵羊精囊丙酮粉形成的多羟基环醚。
Biochemistry. 1971 Sep 28;10(20):3664-9. doi: 10.1021/bi00796a005.
2
A novel prostaglandin derivative formed from arachidonic acid by rat stomach homogenates.一种由大鼠胃匀浆从花生四烯酸形成的新型前列腺素衍生物。
Biochemistry. 1971 Sep 28;10(20):3657-64. doi: 10.1021/bi00796a004.
3
Isolation and properties of intermediates in prostaglandin biosynthesis.前列腺素生物合成中间体的分离与特性
花生四烯酸在大鼠离体灌流心脏中的冠状动脉收缩和舒张作用。
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Cardiovascular risks and benefits of perioperative nonsteroidal anti-inflammatory drug treatment.围手术期非甾体抗炎药治疗的心血管风险与益处
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Biochim Biophys Acta. 1973 Dec 20;326(3):448-61. doi: 10.1016/0005-2760(73)90145-8.
4
Isolation and structure of two prostaglandin endoperoxides that cause platelet aggregation.两种引起血小板聚集的前列腺素内过氧化物的分离与结构
Proc Natl Acad Sci U S A. 1974 Feb;71(2):345-9. doi: 10.1073/pnas.71.2.345.
5
Detection and isolation of an endoperoxide intermediate in prostaglandin biosynthesis.前列腺素生物合成中一种内过氧化物中间体的检测与分离。
Proc Natl Acad Sci U S A. 1973 Mar;70(3):899-903. doi: 10.1073/pnas.70.3.899.
6
Prostaglandin endoperoxides. VII. Novel transformations of arachidonic acid in guinea pig lung.前列腺素内过氧化物。VII. 豚鼠肺中花生四烯酸的新型转化
Biochem Biophys Res Commun. 1974 Dec 11;61(3):942-9. doi: 10.1016/0006-291x(74)90246-0.
7
Thromboxanes: a new group of biologically active compounds derived from prostaglandin endoperoxides.血栓素:一类从前列腺素内过氧化物衍生而来的新型生物活性化合物。
Proc Natl Acad Sci U S A. 1975 Aug;72(8):2994-8. doi: 10.1073/pnas.72.8.2994.
8
Thromboxane A2 and prostaglandin H2: potent stimulators of the swine coronary artery.血栓素A2和前列腺素H2:猪冠状动脉的强效刺激物。
Prostaglandins. 1976 Dec;12(6):943-50. doi: 10.1016/0090-6980(76)90128-3.
9
Arterial walls generate from prostaglandin endoperoxides a substance (prostaglandin X) which relaxes strips of mesenteric and coeliac ateries and inhibits platelet aggregation.动脉壁从前列腺素内过氧化物生成一种物质(前列腺素X),该物质可使肠系膜动脉和腹腔动脉条松弛,并抑制血小板聚集。
Prostaglandins. 1976 Dec;12(6):897-913. doi: 10.1016/0090-6980(76)90125-8.
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Coronary arterial smooth muscle contraction by a substance released from platelets: evidence that it is thromboxane A2.血小板释放的一种物质引起冠状动脉平滑肌收缩:证据表明该物质是血栓素A2。
Science. 1976 Sep 17;193(4258):1135-7. doi: 10.1126/science.959827.