Inhibitory effect of various thrombin inhibitors on shear-induced platelet function and dynamic coagulation

European Journal of Pharmacology

Volumn 406, Issue 2, 2000, Pages 181-189

  Taka, Tomomi ^a   Konishi, Yasuo ^b   Slon Usakiewicz, Jacek ^b   Medvedkin, Viacheslav ^b   Tsuda, Yuko ^a   Okada, Yoshio ^a   Seki, Junji ^c   Yamamoto, Junichiro ^a  

^a KOBE GAKUIN UNIVERSITY   (Japan)

^b NATIONAL RESEARCH COUNCIL CANADA   (Canada)

^c NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER   (Japan)

Author keywords

Bifunctional inhibitor; Coagulation; Platelet aggregation; Shear; Thrombin

Indexed keywords

ARGATROBAN; P 1053; P 553; P 824; P 891; P 899; P 960; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BLOOD CLOTTING; BLOOD FLOW; FIBRIN CLOT; HEMOSTASIS; PRIORITY JOURNAL; SHEAR STRESS; THROMBOCYTE ADHESION; THROMBOCYTE AGGREGATION; THROMBOCYTE FUNCTION;

ANIMAL; ANTITHROMBINS; BLOOD COAGULATION; BLOOD PLATELETS; FACTOR XA; MALE; PIPECOLIC ACIDS; RATS; RATS, WISTAR; SUPPORT, NON-U.S. GOV'T; THROMBIN;

EID: 0034644826     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(00)00655-5     Document Type: Article

References (44)

1. Antman E.M. Hirudin in acute myocardial infarction: safety report from the thrombolysis and thrombin inhibition in myocardial infarction (TIMI) 9A trial. Circulation. 90:1994;1624-1630. for the TIMI 9A Investigators.
2. Badimon L., Badimon J.J., Lassila R., Heras M., Chesebro J.H., Fuster V. Thrombin regulation of platelet interaction with damaged vessel wall and isolated collagen type I at arterial flow conditions in a porcine model: effects of hirudins, heparin, and calcium chelation. Blood. 78:1991;423-434.
3. Born G.V.R. Aggregation of blood platelets by adenosine diphosphate and its reversal. Nature. 194:1962;927-929.
4. Cattaneo M., Pareti F.I., Zighetti M.L., Lecchi A., Lombardi R., Mannucci P.M. Platelet aggregation at high shear is impaired in patients with congenital defects of platelet secretion and is corrected by DDAVP: correlation with the bleeding time. J. Lab. Clin. Med. 125:1995;540-547.
5. Chow T.W., Hellums J.D., Moake J.L., Kroll M.H. Shear stress-induced von Willebrand factor binding to platelet glycoprotein Ib initiates calcium influx associated with aggregation. Blood. 80:1992;113-120.
6. Connolly T.M., Condra C., Feng D.M., Cook J.J., Stranieri M.T., Reilly C.F., Nutt R.F., Gould R.J. Species variability in platelet and other cellular responsiveness to thrombin receptor-derived peptides. Thromb. Haemostasis. 72:1994;627-633.
7. 45-65. J. Biol. Chem. 265:1990;21698-21703.
8. Fernandez-Ortiz A., Badimon J.J., Falk E., Fuster V., Meyer B., Mailhac A., Weng D., Shah P.K., Badimon L. Characterization of the relative thrombogenicity of atherosclerotic plaque components: implications for consequences of plaque rupture. JACC. 23:1994;1562-1569.
9. Gailani D., Broze G.J. Jr. Factor XI activation in a revised model of blood coagulation. Science. 253:1991;909-912.
10. Gorog D.A., Kovacs I.B. Thrombotic status analyser: measurement of platelet-rich thrombus formation and lysis in native blood. Thromb. Haemostasis. 73:1995;514-520.
11. Gorog P., Kovacs I.B. Modelling coronary thrombosis from nonanticoagulated human blood in vitro. Hematol. Pathol. 4:1990;43-52.
12. Goto S., Sakai H., Goto M., Ono M., Ikeda Y., Handa S., Ruggeri Z.M. Enhanced shear-induced platelet aggregation in acute myocardial infarction. Circulation. 99:1999;608-613.
13. GUSTO IIa Investigators Randomized trial of intravenous heparin versus recombinant hirudin for acute coronary syndromes. Circulation. 90:1994;1631-1637.
14. GUSTO IIb Investigators A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes. N. Engl. J. Med. 335:1996;775-782.
15. Hamburger S.A., McEver R.P. GMP-140 mediates adhesion of stimulated platelets to neutrophils. Blood. 75:1990;550-554.
16. Hara T., Yokoyama A., Ishihara H., Yokoyama Y., Nagahara T., Iwamoto M. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb. Haemostasis. 71:1994;314-319.
17. Harker L.A., Hanson S.R., Runge M.S. Thrombin hypothesis of thrombus generation and vascular lesion formation. Am. J. Cardiol. 75:1995;12B-17B.
18. Ikarugi H., Taka T., Nakajima S., Noguchi T., Watanabe S., Sasaki Y., Haga S., Ueda T., Seki J., Yamamoto J. Norepinephrine, but not epinephrine, enhances platelet reactivity and coagulation after exercise in humans. J. Appl. Physiol. 86:1999;133-138.
19. Ikeda Y., Handa M., Kamata T., Kawano K., Kawai Y., Watanabe K., Kawakami K., Sakai K., Fukuyama M., Itagaki I., Yoshioka A., Ruggeri Z.M. Transmembrane calcium influx associated with von Willebrand factor binding to GP Ib in the initiation of shear-induced platelet aggregation. Thromb. Haemostasis. 69:1993;496-502.
20. Kahn M.L., Zheng Y.W., Huang W., Bigornia V., Zeng D., Moff S., Farese R.V., Tam C., Coughlin S.R. A dual thrombin receptor system for platelet activation. Nature. 394:1998;690-694.
21. Kikumoto R., Tamao Y., Tezuka T., Tonomura S., Hara H., Ninomiya K., Hijikata A., Okamoto S. Selective inhibition of thrombin by (2R, 4R)-4-methyl-1-[N2-(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl]-L-arginyl)]-2-piperidinecarboxylic acid. Biochemistry. 23:1984;85-90.
22. Krstenansky J.L., Broersma R.J., Owen T.J., Payne M.H., Yates M.T., Mao S.J.T. Development of MDL 28,050, a small stable antithrombin agent based on a functional domain of the leech protein, hirudin. Thromb. Haemostasis. 63:1990;208-214.
23. Lopez-Farre A., Riesco A., Digiuni E., Mosquera J.R., Caramelo C., Miguel L.S., Millas I., Frutos T., Cernadas M.R., Monton M., Alonso J., Casado S. Aspirin-stimulated nitric oxide production by neutrophils after acute myocardial ischemia in rabbits. Circulation. 94:1996;83-87.
24. Maraganore J.M., Bourdon P., Jablonski J., Ramachandran K.L., Fenton J.W. II Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin. Biochemistry. 29:1990;7095-7101.
25. Markwardt F. Hirudin and derivatives as anticoagulant agents. Thromb. Haemostasis. 66:1991;141-152.
26. Matsuo T., Koide M., Kario K. Development of argatroban, a direct thrombin inhibitor, and its clinical application. Semin. Thromb. Hemostasis. 23:1997;517-522.
27. Moake J.L. Thrombotic thrombocytopenic purpura. Thromb. Haemostasis. 74:1995;240-245.
28. Mustonen P., Lassila R. Epinephrine augments platelet recruitment to immobilized collagen in flowing blood-evidence for a von Willebrand factor-mediated mechanism. Thromb. Haemostasis. 75:1996;175-181.
29. Oliver J.A., Monroe D.M., Roberts H.R., Hoffman M. Thrombin activates factor XI on activated platelets in the absence of factor XII. Arterioscler., Thromb. Vasc. Biol. 19:1999;170-177.
30. Peters N.S., Abrams L.S.M., Dymond D.S., Kovacs I.B. Platelet hyperreactivity and inefficient spontaneous thrombolysis in patients at high risk from an acute coronary event. Cardiovasc. Res. 23:1989;567-572.
31. Ratnatunga C.P., Edmondson S.F., Rees G.M., Kovacs I.B. High-dose aspirin inhibits shear-induced platelet reaction involving thrombin generation. Circulation. 85:1992;1077-1082.
32. Rydel T.J., Ravichandran K.G., Tulinsky A., Bode W., Huber R., Roitsch C., Fenton J.W. II The structure of a complex of recombinant hirudin and human α-thrombin. Science. 249:1990;277-280.
33. Sakariassen K.S., Ottenhof-Rovers M., Sixma J.J. Factor VIII-von Willebrand factor requires calcium for facilitation of platelet adherence. Blood. 63:1984;996-1003.
34. Sasaki Y., Morii S., Yamashita T., Yamamoto J. Antithrombotic effect of argatroban on the pial vessels of the rat: a study with He-Ne laser-induced thrombus formation. Haemostasis. 23:1993;104-111.
35. Siess W., Zangl K.J., Essler M., Bauer M., Brandl R., Corrinth C., Bittman R., Tigyi G., Aefelbacher M. Lysophosphatidic acid mediates the rapid acivaiton of platelets and endothelial cells by mildly oxidized low density lipoprotein and accumulates in human atherosclerotic lesions. Proc. Natl. Acad. Sci. U. S. A. 96:1999;6931-6936.
36. Sixma J.J. Interaction of blood platelets with the vessel wall. Blood A.S., Forbes C.D., Thomas D.P., Tuddenham E.G.D. Haemostasis and Thrombosis. 1994;259-285 Livingstone, London.
37. Szewczuk Z., Gibbs B.F., Yue S.Y., Purisima E.O., Konishi Y. Conformationally restricted thrombin inhibitors resistant to proteolytic digestion. Biochemistry. 31:1992;9132-9140.
38. Tsuda Y., Cygler M., Gibbs B.F., Pedyczak A., Fethiere J., Yue S.Y., Konishi Y. Design of potent bivalent thrombin inhibitors based on hirudin sequence: incorporation of nonsubstrate-type active site inhibitors. Biochemistry. 33:1994;14443-14451.
39. Uchiyama S., Yamazaki M., Maruyama S., Handa M., Ikeda Y., Fukuyama M., Itagaki I. Shear-induced platelet aggregation in cerebral ischemia. Stroke. 25:1994;1547-1551.
40. Umemura K., Kawai H., Ishihara H., Nakashima M. Inhibitory effect of clopidogrel, vapiprost and argatroban on the middle cerebral artery thrombosis in the rat. Jpn. J. Pharmacol. 67:1995;253-258.
41. Valles J., Santos M.T., Aznar J., Marcus A.J., Martinez-Sales V., Portoles M., Broekman M.J., Safier L.B. Erythrocytes metabolically enhance collagen-induced platelet responsiveness via increased thromboxane production, adenosine diphosphate release, and recruitment. Blood. 78:1991;154-162.
42. Vu T.K.H., Hung D.T., Wheaton V.I., Coughlin S.R. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell. 64:1991;1057-1068.
43. Yamamoto J., Taka T., Nakajima S., Ueda M., Sugimoto E., Sasaki Y., Muraki T., Seki J., Watanabe S. A shear-induced in vitro platelet function test can assess clinically relevant anti-thrombotic effects. Platelets. 10:1999;178-184.
44. Yamashita T., Tsuda Y., Konishi Y., Okada Y., Matsuoka A., Giddings J.C., Yamamoto J. The antithrombotic effect of potent bifunctional thrombin inhibitors based on hirudin sequence, P551 and P532, on He-Ne laser-induced thrombosis in rat mesenteric microvessels. Thromb. Res. 90:1998;199-206.