Antithrombotic actions of selective inhibitors of blood coagulation factor Xa in rat models of thrombosis

Thrombosis Research

Volumn 83, Issue 2, 1996, Pages 117-126

  Wong, Pancras C ^a   Crain Jr , Earl J ^a   Nguan, Oliver ^a   Watson, Carol A ^a   Racanelli, Adrienne ^a  

^a DUPONT COMPANY   (United States)

Author keywords

DX 9065a; factor Xa; heparin; thrombosis; tick anticoagulant peptide

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; HEPARIN; RECOMBINANT TICK ANTICOAGULANT PEPTIDE;

ANIMAL CELL; ANIMAL TISSUE; ANTICOAGULATION; ARTICLE; BLOOD CLOTTING; DOSE RESPONSE; DRUG EFFICACY; DRUG MECHANISM; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; RAT; THROMBOSIS; THROMBOSIS PREVENTION;

EID: 0030586091     PISSN: 00493848     EISSN: None     Source Type: Journal    
DOI: 10.1016/0049-3848(96)00112-0     Document Type: Article

References (23)

1. 1. DAVIE, E.W., FUJIKAWA, K. and KISIEL, W. The coagulation cascade: initiation, maintenance, and regulation. Biochem. 30, 10363-10370, 1991.
2. 2. NEEPER, M.P., WAXMAN, L., SMITH, D.E., SCHULMAN, C.A., SARDINA, M., ELLIS, R.W., SCHAFFER, L.W., SIEGL, P.K.S. and VLASUK, G.P. Characterization of recombinant tick anticoagulant peptide. J. Biol. Chem. 265, 17746-17752, 1990.
3. 3. WAXMAN, L., SMITH, D.E., ARCURI, K.E. and VLASUK, G.P. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science 248, 593-596, 1990.
4. 4. JORDAN, S.P., WAXMAN, L., SMITH, D.E. and VLASUK, G.P. Tick anticoagulant peptide: Kinetic analysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry 291, 11095-11100, 1990.
5. 5. VLASUK, G.P., RAMJIT, D., FUJITA, T., DUNWIDDIE, C.T., NUTT, E.M., SMITH, D.E. and SHEBUSKI, R.J. Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rabbit model of venous thrombosis. Thromb. Haemostas. 65, 257-262, 1991.
6. 6. FIORAVANTI, C., BURKHOLDER, D., FRANCIS, B., SIEGL, P.K.S. and GIBSON, R.E. Antithrombotic activity of recombinant tick anticoagulant peptide and heparin in a rabbit model of venous thrombosis. Thromb. Res. 71, 317-324, 1993.
7. 7. SCHAFFER, L.W., DAVIDSON, J.T., VLASUK, G.P. and SIEGL, P.K.S. Antithrombotic efficacy of recombinant tick anticoagulant peptide. Apotent inhibitor of coagulation factor Xa in a primate model of arterial thrombosis. Circ. 84, 1741-1748, 1991.
8. 8. MELLOTT, M.J., STRANIERI, M.T., SITKO, G.R., STABILITO, I.I., LYNCH, J.J. AND VLASUK, G.P. Enhancement of recombinant tissue plasminogen activator-induced reperfusion by recombinant tick anticoagulant peptide, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombosis. Fibrinolysis 7, 195-202, 1993.
9. 9. LYNCH, J.L., SITKO, G.R., LEHMAN, E.D. and VLASUK, G.P. Primary prevention of coronary arterial thrombosis with the factor Xa inhibitor rTAP in a canine electrolytic injury model. Thromb. Haemostas. 74, 640-645, 1995.
10. 10. HARA, T., YOKOYAMA, A., ISHIHARA, H., YOKOYAMA, Y., NAGAHARA, T. and IWAMOTO, M. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb. Haemostas. 77, 314-319, 1994.
11. 11. HARA, T., YOKOYAMA, A., MORISHIMA, Y. and KUNITADA, S. Species differences in anticoagulant and anti-Xa activity of DX-9065a, a highly selective factor Xa inhibitor. Thromb. Res. 80, 99-104, 1995.
12. 12. NAGAHARA, T., KATAKURA, S., INAMURA, K., KOMORIYA, S., HARA, T., KUNITADA, S., YOKOYAMA, Y., YAMAZAKI, K. and IWAMOTO, M. DX-9065A. Drugs Fut. 20, 564-566, 1995.
13. 13. HARA, T., YOKOYAMA, A., TANABE, K., ISHIHARA, H. and IWAMOTO, M. DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb. Haemostas. 74, 635-639, 1995.
14. 14. YOKOYAMA, T., KELLY, A.B., MARZEC, U.M., HANSON, S.R., KUNITADA, S. and HARKER, L. A. Antithrombotic effects of orally active synthetic antagonist of activated factor X in nonhuman primates. Circ. 92, 485-491, 1995.
15. 15. YAMAZAKI, M., ASAKURA, H., AOSHIMA, K., SAITO, M., JOKAJI, H., UOTANI, C., KUMABASHIRI, I., MORISHITA, E., IKEDA, T. and MATSUDA, T. Effects of DX-9065a, an orally active, newly synthetized and specific inhibitor of factor Xa, against experimental disseminated intravascular coagulation in rats. Thromb. Haemostas. 72, 393-396, 1994.
16. 16. NAGAHARA T., YOKOYAMA, Y., INAMURA, K., KATAKURA, S., KOMORIYA, S., YAMAGUCHI, H., HARA, T. and IWAMOTO, M. DIBASIC (Amidino-aryl)-propanoic acid derivative as novel blood coagulation factor Xa inhibitors. J. Med. Chem. 37, 1200-1207, 1994.
17. 17. BERRY, C.N., GIRARD, D., LOCHOT, S. and LECOFFRE, C. Antithrombotic actions of argatroban in rat models of venous, 'mixed' and arterial thrombosis, and its effects on the tail transaction blood ing time. Br. J. Pharmacol. 113, 1209-1214, 1994.
18. 18. PETERS, R.F., LEES, C.M., MITCHELL, K.A., TWEED, M.F., TALBOT, M.D. and WALLIS, R.B. The characterization of thrombus development in an improved model of arteriovenous thrombosis in the rat and the effects of recombinant desulphatohirudin (CGP 39393), heparin, and iloprost. Thromb. Haemostas. 65, 268-274, 1991.
19. 19. HLADOVEC, J. Antithrombotics in view of thrombosis models. Thromb. Res. 43, 545-551, 1986.
20. 20. KNABB, R.M., KETTNER, C.A., TIMMERMANS, P.B.M.W.M. and REILLY, T.M. In vivo characterization of a new synthetic thrombin inhibitor. Thromb. Haemostas. 67: 56-59, 1992.
21. 21. CODY, R.P. and SMITH, J.K. Applied statistics and the SAS programming language., 2nd ed. Elsevier Science, New York (1987).
22. 22. VOGEL, G.M.T., MEULEMAN, D.G., BOURGONDIEN, F.G.M. and HOBBELEN, P.M.J. Comparison of two experimental thrombosis models in rats effects of four glycosaminoglycans. Thromb. Res. 54, 399-410, 1989.
23. 23. DUNWIDDIE, C.T., SMITH, D.E., NUTT, E.M. and VLASUK, G.P. Anticoagulant effects of the selective factor Xa inhibitors tick anticoagulant peptide and antisasin in the APTT assay are determined by the relative rate of prothrombinase inhibition. Thromb. Res. 64, 787-794, 1991.