Antithrombotic effects of YM-60828, a newly synthesized factor Xa inhibitor, in rat thrombosis models and its effects on bleeding time

British Journal of Pharmacology

Volumn 123, Issue 1, 1998, Pages 92-96

  Sato, Kazuo ^a   Kawasaki, Tomihisa ^a   Hisamichi, Nami ^a   Taniuchi, Yuta ^a   Hirayama, Fukushi ^a   Koshio, Hiroyuki ^a   Matsumoto, Yuzo ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

Argatroban; Arterio venous shunt; Bleeding time; Dalteparin; Heparin; Venous thrombosis; YM 60828

Indexed keywords

[N [4 [(1 ACETIMIDOYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL]ACETIC ACID; ANTICOAGULANT AGENT; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; DALTEPARIN; HEPARIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERIOVENOUS SHUNT; ARTICLE; BLEEDING TIME; CONTROLLED STUDY; DOSE RESPONSE; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; PROTHROMBIN TIME; RAT; VEIN THROMBOSIS;

ANIMALS; ANTICOAGULANTS; ARTERIOVENOUS SHUNT, SURGICAL; BLEEDING TIME; BLOOD PROTEINS; DALTEPARIN; FACTOR XA; FIBRINOLYTIC AGENTS; HEPARIN; MALE; NAPHTHALENES; PARTIAL THROMBOPLASTIN TIME; PIPECOLIC ACIDS; PIPERIDINES; PLATELET AGGREGATION INHIBITORS; RATS; RATS, SPRAGUE-DAWLEY; THROMBOPHLEBITIS; THROMBOSIS;

EID: 0031964032     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701566     Document Type: Article

References (22)

1. ANDERSSON, L.O., BARROWCLIFFE, T.W., HOLMER, E., JOHNSON, E.A. & SOLDERSTROM, G. (1979). Molecular weight dependency of the heparin potentiated inhibition of thrombin and activated factor X. Effect of heparin neutralization in plasma. Thromb. Res., 15, 531-541.
2. BERNDT, M.C., GREGORY, C., DOWDEN, G. & CASTALDI, P.A. (1986). Thrombin interaction with platelet membrane proteins. Ann. New York Acad. Sci., 485, 374-386.
3. BERRY, C.N., GIRARD, D., LOCHOT, S. & LECOFFRE, C. (1994). Antithrombotic actions of argatroban in rat models of venous, mixed' and arterial thrombosis, and its effects on the tail transection bleeding time. Br. J. Pharmacol., 113, 1209-1214.
4. CARTER, C.J., KELTON, J.G., HIRSH, J., CERSKUS, A., SANTOS, A.V. & GENT, M. (1982). The relationship between the hemorrhagic and antithrombotic properties of low molecular weight heparin in rabbits. Blood, 59, 1239-1245.
5. HAMANO, S., KOMATSU, H., IKEDA, S., TAKAHASHI, K., OGUMA, Y. & SAKURAGAWA, N. (1989). Beneficial effect of low molecular weight heparin on the hemodialysis model in dogs. Thromb. Res., 55, 439-449.
6. HAMANO, S., NISHIYAMA, M., KOMATSU, H., MIYATA, H., IKEDA, S. & SAKURAGAWA, N. (1992). Study of anticoagulant mechanism of low molecular weight heparin. Thromb. Res., 65, 801-808.
7. HARA, T., YOKOYAMA, A., TANABE, K., ISHIHARA, H. & IWAMOTO, M. (1995). DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb. Haemost., 74, 635-639.
8. HERBERT, J.M., BERNAT, A., DOL, F., HERAULT, J.P., CREPON, B. & LOKMEAU, J.C. (1996). DX 9065A, a novel, synthetic, selective and orally active inhibitor of factor Xa: in vitro and in vivo studies. J. Pharmacol. Exp. Ther., 276, 1030-1038.
9. HIGGINS, D.L., LEWIS, S.D. & SHAFER, J.A. (1983). Steady state kinetic parameters for the thrombin catalyzed conversion of human fibrinogen to fibrin. J. Biol. Chem., 258, 9276-9282.
10. HOLMER, E., MATTSON, C. & NILSSON, S. (1982). Anticoagulant and antithrombotic effects of herapin and low molecular weight heparin fragments in rabbits. Thromb. Res., 25, 475-485.
11. IMURA, Y., STASSEN, J.M. & COLLEN, D. (1992). Comparative antithrombotic effects of heparin, recombinant hirudin and argatroban in a hamster femoral vein platelet-rich mural thrombosis model. J. Pharmacol. Exp. Ther., 261, 895-898.
12. LEFKOVITS, J. & TOPOL, E.J. (1994). Direct thrombin inhibitors in cardiovascular medicine. Circulation, 90, 1522-1536.
13. MACDONALD, J.D., REMINGTON, B.J. & RODGERS, G.M. (1994). The skin bleeding time test as a predictor of brain bleeding time in a rat model. Thromb. Res., 76, 535-540.
14. NEEPER, M.P., WAXMAN, L., SMITH, D.E., SCHULMAN, C.A., SARDANA, M., ELLIS, R.W., SCHAFFER, L.W., SIEGEL, P.K. & VLASUK, G.P. (1990). Characterization of recombinant tick anticoagulant peptide. A highly selective inhibitor of blood coagulation factor Xa. J. Biol. Chem., 265, 17746-17752.
15. OKAMOTO, S., HIJIKATA, A., KIKUMOTO, R., TONOMURA, S., HARA, H., NINOMIYA, K., MARUYAMA, A., SUGANO, M. & TAMAO, Y. (1981). Potent inhibition of thrombin by the newly synthesized arginine derivative No. 805. The importance of stereo-structure of its hydrophobic carboxamide portion. Biochem. Biophys. Res. Commun., 101, 440-446.
16. PETERS, R.F., LEES, C.M., MITCHELL, K.A., TWEED, M.F., TALBOT, M.D. & WALLIS, R.H. (1991). The characterization of thrombus development in an improved model of arterio-venous shunt thrombosis in the rat and the effects of recombinant desulphatohirudin (CGP 39393), heparin, and iloprost. Thromb. Haemost., 65, 268-274.
17. REYERS, I., MUSSONI, L., DONATI, M.B. & DE GAETANO, G. (1980). Failure of aspirin at different doses to modify experimental thrombosis in rats. Thromb. Res., 18, 669-674.
18. ROSENBERG, J.S., BEELER, D.L. & ROSENBERG, R.D. (1975). Activation of human prothrombin by highly purified human factors V and Xa in presence of human antithrombin. J. Biol. Chem., 250, 1607-1617.
19. ROSENBERG, R.D. & DAMUS, P.S. (1973). Purification and mechanism of action of human antithrombm-heparin cofactor. J. Biol. Chem., 248, 6498-6505.
20. SCHAFFER, L.W., DAVIDSON, J.T., SIEGL, P.K., GOULD, R.J., NUTT, R.F., BRADY, S.F. & CONNOLLY, T.M. (1993). Selective factor Xa inhibition by recombmant antistasin prevents vascular graft thrombosis in baboons. Arterioscler. Thromb., 12, 879-885.
21. SITKO, G.R., RAMJIT, D.R. STABILITO, I.I., LEHMAN, D., LYNCH, J.L. & VLASUK, G.P. (1992). Conjunctive enhancement of enzymatic thrombolysis and prevention of thrombotic reocclusion with the selective factor Xa inhibitor, tick anticoagulant peptide. Circulation, 85, 805-815.
22. YAMAZAKI, M., ASAKURA, H., AOSHIMA, K., SAITO, M., JOKAJI, H., UOTANI, C., KUMABASHIRI, I., MORISHITA, E., IKEDA, T. & MATSUDA, T. (1994). Effects of DX-9065a, an orally active, newly synthesized and specific inhibitor of factor Xa, against experimental disseminated intravascular coagulation in rats. Thromb. Haemost., 72, 393-396.