Inhibition of Platelet Aggregation and Cardiovascular Effect of 5E-13,14-Didehydro Carboprostacyclin and 5E-13,14-Didehydro-20-Methyl-Carboprostacyclin
After the discovery of prostacyclin (PGI2) in 1976 , the most potent inhibitor of human platelet aggregation in vitro  with simultaneous strong hypotensive effect in animals and humans [1, 2, 3], many efforts have been made to synthesize PGI2-derivatives that are chemically stable and which possibly have longer lasting action. The first goal has been reached easily enough and carboprostacyclin [4, 5], 10,10-difluoro-13,14-dehydroprostacyclin  and 16-methyl-18 yl carboprostacyclin (ZK-36374)  are the best known results of these efforts.
KeywordsPlatelet Aggregation Arterial Blood Pressure Pulmonary Arterial Pressure Part Blood Bovine Coronary Artery
Unable to display preview. Download preview PDF.
- 3.A. Szczeklik, R. J. Gryglewski, R. Nizankowski, J. Musial, R. Pieton, and J. Mruk, Circulatory and antiplatelet effects of intravenous prostacyclin in healthy man, Pharm. Res. Commun., 10: 545 (1978).Google Scholar
- 5.R. Ceserani, M. Grossoni, D. Longiave, B. Mizzotti, 0. Pozzi, A. Dembinska-Kiec’, and S. Bianco, dl-9a-deoxy-9a-methylenePGI2 (a stable prostacyclin derivative): preliminary pharmacological data, Prostaglandins and Medicine, 5: 131 (1980).Google Scholar
- 7.K. Schrdr, H. Darius, R. Matzky, and R. Ohlendorf, The anti-platelet and cardiovascular actions of a new carbacyclin derivative (ZK 36374) equipotent to PGI2 in vitro, Naunyn-Schmiedeberg’s Arch. Pharmacol., 316: 252 (1981).Google Scholar
- 8.R. Ceserani, D. Longiave, M. Grossoni, M. Bergamaschi, C. Gondolfi, N. Mongelli, and L. Zuliani, 5E-13,14-didehydrocarboprostacyclin and 5E-13,14-didehydro-20-methyl-carboprostacyclin: preliminary data on inhibition of platelet aggregation and hypotensive effect, IRCS Medical Sciences, 9: 364 (1981).Google Scholar
- 9.D. J. Finney, Statistical Methods in Biological Assay (C. Griffin, ed. ), London (1972).Google Scholar
- 10.H. Grimm, Principles of statistical estimation, in: “Biostatistics in Pharmacology,” Vol. 2 (A. L. Delaunois, ed.), Pergamon Press, Ltd., Oxford, p. 611 (1973).Google Scholar
- 11.B. J. R. Baley, Tables of the Bonferroni “t” statistic, J.A.S.A. Vol. 72, No. 358, p. 469 (1977).Google Scholar