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. 1980 Jan 26;122(2):175–179.

Prostaglandin I2 (prostacyclin).

J G Kelton, M A Blajchman
PMCID: PMC1801769  PMID: 6988063

Abstract

Prostaglandin I2 (PGI2), or prostacyclin, is a recently discovered prostaglandin that affects many organ systems. It is both a potent inhibitor of platelet aggregation and a powerful vasodilator. The recent demonstration that it is the main prostaglandin synthesized by the blood vessel wall suggests that it may play an important role in limiting platelet-mediated thrombosis. However, despite considerable investigation, the exact physiological role of PGI2 has yet to be elucidated.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Baenziger N. L., Dillender M. J., Majerus P. W. Cultured human skin fibroblasts and arterial cells produce a labile platelet-inhibitory prostaglandin. Biochem Biophys Res Commun. 1977 Sep 9;78(1):294–301. doi: 10.1016/0006-291x(77)91253-0. [DOI] [PubMed] [Google Scholar]
  2. Blajchman M. A., Senyi A. F., Hirsh J., Surya Y., Buchanan M., Mustard J. F. Shortening of the bleeding time in rabbits by hydrocortisone caused by inhibition of prostacyclin generation by the vessel wall. J Clin Invest. 1979 May;63(5):1026–1035. doi: 10.1172/JCI109371. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Bunting S., Moncada S., Vane J. R. Antithrombotic properties of vascular endothelium. Lancet. 1977 Nov 19;2(8047):1075–1076. doi: 10.1016/s0140-6736(77)91906-7. [DOI] [PubMed] [Google Scholar]
  4. Dembinska-Kiec A., Gryglewska T., Zmuda A., Gryglewski R. J. The generation of prostacyclin by arteries and by the coronary vascular bed is reduced in experimental atherosclerosis in rabbits. Prostaglandins. 1977;14(6):1025–1034. doi: 10.1016/0090-6980(77)90282-9. [DOI] [PubMed] [Google Scholar]
  5. Deykin D. Emerging concepts of platelet function. N Engl J Med. 1974 Jan 17;290(3):144–151. doi: 10.1056/NEJM197401172900308. [DOI] [PubMed] [Google Scholar]
  6. Dusting G. J., Moncada S., Vane J. R. Prostacyclin (PGX) is the endogenous metabolite responsible for relaxation of coronary arteries induced by arachindonic acid. Prostaglandins. 1977 Jan;13(1):3–15. doi: 10.1016/0090-6980(77)90037-5. [DOI] [PubMed] [Google Scholar]
  7. Gorman R. R., Bunting S., Miller O. V. Modulation of human platelet adenylate cyclase by prostacyclin (PGX). Prostaglandins. 1977 Mar;13(3):377–388. doi: 10.1016/0090-6980(77)90018-1. [DOI] [PubMed] [Google Scholar]
  8. Gryglewski R. J., Bunting S., Moncada S., Flower R. J., Vane J. R. Arterial walls are protected against deposition of platelet thrombi by a substance (prostaglandin X) which they make from prostaglandin endoperoxides. Prostaglandins. 1976 Nov;12(5):685–713. doi: 10.1016/0090-6980(76)90047-2. [DOI] [PubMed] [Google Scholar]
  9. Gryglewski R. J., Korbut R., Ocetkiewicz A. De-aggregatory action of prostacyclin in vivo and its enhancement by theophylline. Prostaglandins. 1978 Apr;15(4):637–644. doi: 10.1016/0090-6980(78)90059-x. [DOI] [PubMed] [Google Scholar]
  10. Hawkings H. J., Smith J. B., Nicolaou K. C., Eling T. E. Studies of the mechanisms involved in the fate of prostacyclin (PGI2) and 6-keto-PGF1alpha in the pulmonary circulation. Prostaglandins. 1978 Dec;16(6):871–884. doi: 10.1016/0090-6980(78)90103-x. [DOI] [PubMed] [Google Scholar]
  11. Henry R. L. Platelet function. Semin Thromb Hemost. 1977 Fall;4(2):93–122. doi: 10.1055/s-0028-1087130. [DOI] [PubMed] [Google Scholar]
  12. Heyns A. P., van den Berg D. J., Potgieter G. M., Retief F. P. The inhibition of platelet aggregation by an aorta intima extract. Thromb Diath Haemorrh. 1974 Dec 31;32(2-3):417–431. [PubMed] [Google Scholar]
  13. Higgs E. A., Higgs G. A., Moncada S., Vane J. R. Prostacyclin (PGI2) inhibits the formation of platelet thrombi in arterioles and venules of the hamster cheek pouch. Br J Pharmacol. 1978 Jul;63(3):535–539. doi: 10.1111/j.1476-5381.1978.tb07809.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Higgs E. A., Moncada S., Vane J. R., Caen J. P., Michel H., Tobelem G. Effect of prostacyclin (PGI2) on platelet adhesion to rabbit arterial subendothelium. Prostaglandins. 1978 Jul;16(1):17–22. doi: 10.1016/0090-6980(78)90197-1. [DOI] [PubMed] [Google Scholar]
  15. Hirsh J., Doery J. C. Platelet function in health and disease. Prog Hematol. 1971;7:185–234. [PubMed] [Google Scholar]
  16. Hornstra G., Haddeman E., Don J. A. Some investigations into the role of prostacyclin in thromboregulation. Thromb Res. 1978 Feb;12(2):367–374. doi: 10.1016/0049-3848(78)90308-0. [DOI] [PubMed] [Google Scholar]
  17. Kelton J. G., Hirsh J., Carter C. J., Buchanan M. R. Thrombogenic effect of high-dose aspirin in rabbits. Relationship to inhibition of vessel wall synthesis of prostaglandin I2-like activity. J Clin Invest. 1978 Oct;62(4):892–895. doi: 10.1172/JCI109203. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Komoriya K., Ohmori H., Azuma A., Kurozumi S., Hashimoto Y., Nicolaou K. C., Barnette W. E., Magolda R. L. Prostaglandin I2 as a potentiator of acute inflammation in rats. Prostaglandins. 1978 Apr;15(4):557–564. doi: 10.1016/0090-6980(78)90052-7. [DOI] [PubMed] [Google Scholar]
  19. MacIntyre D. E., Pearson J. D., Gordon J. L. Localisation and stimulation of prostacyclin production in vascular cells. Nature. 1978 Feb 9;271(5645):549–551. doi: 10.1038/271549a0. [DOI] [PubMed] [Google Scholar]
  20. Marcus A. J., Weksler B. B., Jaffe E. A. Enzymatic conversion of prostaglandin endoperoxide H2 and arachidonic acid to prostacyclin by cultured human endothelial cells. J Biol Chem. 1978 Oct 25;253(20):7138–7141. [PubMed] [Google Scholar]
  21. Mathé A. A., Hedqvist P., Strandberg K., Leslie C. A. Aspects of prostaglandin function in the lung (first of two parts). N Engl J Med. 1977 Apr 14;296(15):850–855. doi: 10.1056/NEJM197704142961505. [DOI] [PubMed] [Google Scholar]
  22. Mills D. C., Macfarlane D. E. Stimulation of human platelet adenylate cyclase by prostaglandin D2. Thromb Res. 1974 Sep;5(3):401–412. doi: 10.1016/0049-3848(74)90176-5. [DOI] [PubMed] [Google Scholar]
  23. Mills D. C., Smith J. B. The influence on platelet aggregation of drugs that affect the accumulation of adenosine 3':5'-cyclic monophosphate in platelets. Biochem J. 1971 Jan;121(2):185–196. doi: 10.1042/bj1210185. [DOI] [PMC free article] [PubMed] [Google Scholar]
  24. Moncada S., Gryglewski R., Bunting S., Vane J. R. An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation. Nature. 1976 Oct 21;263(5579):663–665. doi: 10.1038/263663a0. [DOI] [PubMed] [Google Scholar]
  25. Moncada S., Herman A. G., Higgs E. A., Vane J. R. Differential formation of prostacyclin (PGX or PGI2) by layers of the arterial wall. An explanation for the anti-thrombotic properties of vascular endothelium. Thromb Res. 1977 Sep;11(3):323–344. doi: 10.1016/0049-3848(77)90185-2. [DOI] [PubMed] [Google Scholar]
  26. Moncada S., Higgs E. A., Vane J. R. Human arterial and venous tissues generate prostacyclin (prostaglandin x), a potent inhibitor of platelet aggregation. Lancet. 1977 Jan 1;1(8001):18–20. doi: 10.1016/s0140-6736(77)91655-5. [DOI] [PubMed] [Google Scholar]
  27. Moncada S., Vane J. R. Arachidonic acid metabolites and the interactions between platelets and blood-vessel walls. N Engl J Med. 1979 May 17;300(20):1142–1147. doi: 10.1056/NEJM197905173002006. [DOI] [PubMed] [Google Scholar]
  28. Moncada S., Vane J. R., Whittle B. J. Relative potency of prostacyclin, prostaglandin E1 and D2 as inhibitors of platelet aggregation in several species [proceedings]. J Physiol. 1977 Dec;273(2):2P–4P. [PubMed] [Google Scholar]
  29. Needleman P., Kaley G. Cardiac and coronary prostaglandin synthesis and function. N Engl J Med. 1978 May 18;298(20):1122–1128. doi: 10.1056/NEJM197805182982005. [DOI] [PubMed] [Google Scholar]
  30. Needleman P. Prostacyclin in blood vessel-platelet interactions: perspectives and questions. Nature. 1979 May 3;279(5708):14–15. doi: 10.1038/279014a0. [DOI] [PubMed] [Google Scholar]
  31. Needleman P., Wyche A., Raz A. Platelet and blood vessel arachidonate metabolism and interactions. J Clin Invest. 1979 Feb;63(2):345–349. doi: 10.1172/JCI109309. [DOI] [PMC free article] [PubMed] [Google Scholar]
  32. Nicolaou K. C., Barnette W. E., Gasic G. P., Magolda R. L. 6,9-thiaprostacyclin. A stable and biologically potent analogue of prostacyclin (PGI2) J Am Chem Soc. 1977 Nov 9;99(23):7736–7738. doi: 10.1021/ja00465a070. [DOI] [PubMed] [Google Scholar]
  33. Omini C., Pasargiklian R., Folco G. C., Fano M., Berti F. Pharmacological activity of PGI2 and its metabolite 6-oxo-PGF1alpha on human uterus and fallopian tubes. Prostaglandins. 1978 Jun;15(6):1045–1054. doi: 10.1016/0090-6980(78)90047-3. [DOI] [PubMed] [Google Scholar]
  34. Pace-Asciak C. R., Carrara M. C., Nicolaou K. C. Prostaglandin I2 has more potent hypotensive properties than prostaglandin E2 in the normal and spontaneously hypertensive rat. Prostaglandins. 1978 Jun;15(6):999–1003. doi: 10.1016/0090-6980(78)90042-4. [DOI] [PubMed] [Google Scholar]
  35. Piper P. J. Introduction to the biosynthesis and metabolism of prostaglandins. Postgrad Med J. 1977 Nov;53(625):643–646. doi: 10.1136/pgmj.53.625.643. [DOI] [PMC free article] [PubMed] [Google Scholar]
  36. Rosenblum W. I., El-Sabban F. Enhancement of platelet aggregation by tranylcypromine in mouse cerebral microvessels. Circ Res. 1978 Aug;43(2):238–241. doi: 10.1161/01.res.43.2.238. [DOI] [PubMed] [Google Scholar]
  37. Santoro S. A., Cunningham L. W. Collagen-mediated platelet aggregation. Evidence for multivalent interactions of intermediate specificity between collagen and platelets. J Clin Invest. 1977 Nov;60(5):1054–1060. doi: 10.1172/JCI108856. [DOI] [PMC free article] [PubMed] [Google Scholar]
  38. Schölkens B. A., Bartmann W., Beck G., Lerch U., Konz E., Weithmann U. Vasodilation and inhibition of platelet aggregation by prostacyclins with modified omega-side chain. Prostaglandins Med. 1979 Jul;3(1):7–22. doi: 10.1016/0161-4630(79)90011-9. [DOI] [PubMed] [Google Scholar]
  39. Silberbauer K., Sinzinger H., Winter M., Feigl W., Ring F. Prostacyclin-like activity of endothelium and subendothelium - important for atherosclerosis? Experientia. 1978 Nov 15;34(11):1471–1472. doi: 10.1007/BF01932360. [DOI] [PubMed] [Google Scholar]
  40. Silberbauer K., Sinzinger H., Winter M. Prostacyclin production by vascular smooth-muscle cells. Lancet. 1978 Jun 24;1(8078):1356–1357. doi: 10.1016/s0140-6736(78)92423-6. [DOI] [PubMed] [Google Scholar]
  41. Szczeklik A., Nizankowski R., Skawinski S., Szczeklik J., Gluszko P., Gryglewski R. J. Successful therapy of advanced arteriosclerosis obliterans with prostacyclin. Lancet. 1979 May 26;1(8126):1111–1114. doi: 10.1016/s0140-6736(79)91792-6. [DOI] [PubMed] [Google Scholar]
  42. Vermylen J., Chamone D. A., Verstraete M. Stimulation of prostacyclin release from vessel wall by Bay g 6575, an antithrombotic compound. Lancet. 1979 Mar 10;1(8115):518–520. doi: 10.1016/s0140-6736(79)90944-9. [DOI] [PubMed] [Google Scholar]
  43. Villa S., Callioni A., de Gaetano G. Normal prostacyclin-like activity in vascular tissues from thrombocytopenic rats. Thromb Res. 1977 Dec;11(6):701–704. doi: 10.1016/0049-3848(77)90098-6. [DOI] [PubMed] [Google Scholar]
  44. Villa S., Mysliwiec M., de Galtano G. Prostacyclin and atherosclerosis in rats. Lancet. 1977 Jun 4;1(8023):1216–1217. doi: 10.1016/s0140-6736(77)92767-2. [DOI] [PubMed] [Google Scholar]
  45. Weeks J. R. The general pharmacology of prostacyclin (pgi2, pgx): a new prostaglandin especially activity on the cardiovascular system. Pol J Pharmacol Pharm. 1978 Mar-Jun;30(2-3):215–221. [PubMed] [Google Scholar]
  46. Weiss H. J., Turitto V. T. Prostacyclin (prostaglandin I2, PGI2) inhibits platelet adhesion and thrombus formation on subendothelium. Blood. 1979 Feb;53(2):244–250. [PubMed] [Google Scholar]
  47. Weksler B. B., Ley C. W., Jaffe E. A. Stimulation of endothelial cell prostacyclin production by thrombin, trypsin, and the ionophore A 23187. J Clin Invest. 1978 Nov;62(5):923–930. doi: 10.1172/JCI109220. [DOI] [PMC free article] [PubMed] [Google Scholar]
  48. Weksler B. B., Marcus A. J., Jaffe E. A. Synthesis of prostaglandin I2 (prostacyclin) by cultured human and bovine endothelial cells. Proc Natl Acad Sci U S A. 1977 Sep;74(9):3922–3926. doi: 10.1073/pnas.74.9.3922. [DOI] [PMC free article] [PubMed] [Google Scholar]

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