Reorientation of prostaglandin endoperoxide metabolism by a thromboxane synthetase inhibitor: in vitro and clinical observations.

作者: J Vermylen , H Deckmyn

DOI: 10.1111/J.1365-2125.1983.TB02102.X

关键词: PlateletInternal medicineThromboxane receptorProstacyclinBiologyThromboxaneIn vivoThromboxane-A synthaseDazoxibenThromboxane A2Endocrinology

摘要: 1 Work with dazoxiben in vitro and vivo suggests that a diminished capacity of platelets to synthesize thromboxane A2 results reorientation the metabolism cyclic endoperoxides. 2 Platelets patients congenital synthetase deficiency show same phenomenon. 3 In presence endothelium or leukocytes which have prostacyclin capacity, significant amounts can be generated if synthesis is blocked. 4 The local generation aggregation inhibiting prostaglandins areas vascular damage may an interesting therapeutic concept. 5 Pilot clinical studies inhibitor (UK 37248) small number peripheral arterial disease did not reveal major consistent haemodynamic changes. 6 Attention directed towards optimizing pharmacologically efficacy inhibitory produced when inhibited.

参考文章(7)
Thomas C Detwiler, Israel F Charo, Richard D Feinman, Evidence that calcium regulates platelet function. Thrombosis and Haemostasis. ,vol. 40, pp. 207- 211 ,(1978) , 10.1055/S-0038-1648653
G. Defreyn, S. J. Machin, L. O. Carreras, M. Vergara Dauden, D. A. F. Chamone, J. Vermylen, Familial Bleeding Tendency with Partial Platelet Thromboxane Synthetase Deficiency: Reorientation of Cyclic Endoperoxide Metabolism British Journal of Haematology. ,vol. 49, pp. 29- 41 ,(1981) , 10.1111/J.1365-2141.1981.TB07194.X
R. Käser-Glanzmann, M. Jakábová, J.N. George, E.F. Lüscher, Stimulation of calcium uptake in platelet membrane vesicles by adenosine 3′,5′-cyclic monophosphate and protein kinase Biochimica et Biophysica Acta (BBA) - Biomembranes. ,vol. 466, pp. 429- 440 ,(1977) , 10.1016/0005-2736(77)90336-4
J VERMYLEN, Thromboxane synthetase inhibition as antithrombotic strategy. The Lancet. ,vol. 317, pp. 1073- 1075 ,(1981) , 10.1016/S0140-6736(81)92241-8
HeywoodM. Tyler, CraigA.P.D. Saxton, M.John Parry, ADMINISTRATION TO MAN OF UK-37,248-01, A SELECTIVE INHIBITOR OF THROMBOXANE SYNTHETASE The Lancet. ,vol. 317, pp. 629- 632 ,(1981) , 10.1016/S0140-6736(81)91551-8
R R Gorman, O V Miller, Evidence for distinct prostaglandin I2 and D2 receptors in human platelets. Journal of Pharmacology and Experimental Therapeutics. ,vol. 210, pp. 134- 140 ,(1979)