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Volumn 7, Issue 6, 1996, Pages 455-458

Argatroban: A synthetic thrombin inhibitor of low relative molecular mass

Author keywords

argatroban; thrombin; thrombin inhibitor; thrombosis

Indexed keywords

ARGATROBAN; THROMBIN INHIBITOR;

EID: 0029783476     PISSN: 09546928     EISSN: None     Source Type: Journal    
DOI: 10.1097/00019501-199606000-00008     Document Type: Review
Times cited : (49)

References (33)
  • 1
    • 0021327417 scopus 로고
    • 2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl]-L-arginyl]-2- piperidinecarboxylic acid
    • 2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl]-L-arginyl]-2- piperidinecarboxylic acid. Biochemistry 1984, 23:85-90. Description of argatroban and its isomers, their activity against thrombin relative to other senne proteases, and of potential interaction with thrombin.
    • (1984) Biochemistry , vol.23 , pp. 85-90
    • Kikumoto, R.1    Tamao, Y.2    Tezuka, T.3    Tonomura, S.4    Hara, H.5    Ninomiya, K.6
  • 2
    • 0025837452 scopus 로고
    • Crystallographic analysis at 3.0-Å resolution of the binding to human thrombin of four active site-directed inhibitors
    • Banner DW, Hadvary P: Crystallographic analysis at 3.0-Å resolution of the binding to human thrombin of four active site-directed inhibitors. J Biol Chem 1991, 266:20085-20093. X-ray crystallography of argatroban-thrombin complex and discussion of the mechanism of specificity.
    • (1991) J Biol Chem , vol.266 , pp. 20085-20093
    • Banner, D.W.1    Hadvary, P.2
  • 3
    • 0025175641 scopus 로고
    • Geometry of binding of the benzamadine- and arginine-based inhibitors N alpha-(2-naphthyl-sulphonyl-glycyl)-DL-p-amidinophenylalanyl-piperidine (NAPAP) and (2R,4R)-4-methyl-1-[N alpha-(3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2- piperidinecarboxylic acid (MQPA) to human alpha-thrombin
    • X-ray Crystallographic determination of the NAPAP-trypsin complex and modeling of NAPAP-thrombin and MQPA-thrombin
    • Bode W, Turk D, Sturzebecher J: Geometry of binding of the benzamadine- and arginine-based inhibitors N alpha-(2-naphthyl-sulphonyl-glycyl)-DL-p-amidinophenylalanyl-piperidine (NAPAP) and (2R,4R)-4-methyl-1-[N alpha-(3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2- piperidinecarboxylic acid (MQPA) to human alpha-thrombin. X-ray Crystallographic determination of the NAPAP-trypsin complex and modeling of NAPAP-thrombin and MQPA-thrombin. Eur J Biochem 1990, 193:175-182. X-ray crystallography of argatroban-thrombin complex and discussion of the mechanism of specificity.
    • (1990) Eur J Biochem , vol.193 , pp. 175-182
    • Bode, W.1    Turk, D.2    Sturzebecher, J.3
  • 4
    • 0019891328 scopus 로고
    • Potent inhibition of thrombin by the newly synthesized arginine derivatives No. 805. The importance of stereo structure of its hydrophobic carboxamide portion
    • Okamoto S, Hijikata A, Kikumoto R, Tonomura S, Hara H, Nonomiya K, et al.: Potent inhibition of thrombin by the newly synthesized arginine derivatives No. 805. The importance of stereo structure of its hydrophobic carboxamide portion. Biochem Biophys Res Commun 1981, 101:440-446.
    • (1981) Biochem Biophys Res Commun , vol.101 , pp. 440-446
    • Okamoto, S.1    Hijikata, A.2    Kikumoto, R.3    Tonomura, S.4    Hara, H.5    Nonomiya, K.6
  • 5
    • 0025155792 scopus 로고
    • Effect of a synthetic thrombin-inhibitor MD 805 on the reaction between thrombin and plasma antithrombin III
    • Hijikata-Okunomiya A, Okamoto S, Wanaka K: Effect of a synthetic thrombin-inhibitor MD 805 on the reaction between thrombin and plasma antithrombin III. Thromb Res 1990, 59:967-977.
    • (1990) Thromb Res , vol.59 , pp. 967-977
    • Hijikata-Okunomiya, A.1    Okamoto, S.2    Wanaka, K.3
  • 6
    • 0029065197 scopus 로고
    • Comparative studies on the anticoagulant and protease generation inhibitory actions of newly developed site-directed thrombin inhibitory drugs. Efegatran, argatroban, hirulog and hirudin
    • Callas DD, Hoppensteadt D, Fareed J: Comparative studies on the anticoagulant and protease generation inhibitory actions of newly developed site-directed thrombin inhibitory drugs. Efegatran, argatroban, hirulog and hirudin. Sem Thromb Hemost 1995, 21:177-183.
    • (1995) Sem Thromb Hemost , vol.21 , pp. 177-183
    • Callas, D.D.1    Hoppensteadt, D.2    Fareed, J.3
  • 7
    • 0026014710 scopus 로고
    • Comparative study of the in vitro effectiveness of antithrombotic agents
    • Paques EP, Romisch J: Comparative study of the in vitro effectiveness of antithrombotic agents. Thromb Res 1991, 64:11-21.
    • (1991) Thromb Res , vol.64 , pp. 11-21
    • Paques, E.P.1    Romisch, J.2
  • 8
    • 0027959329 scopus 로고
    • Effects of the synthetic thrombin inhibitor argatroban on fibrin- Or clot-incorporated thrombin: Comparison with heparin and recombinant hirudin
    • Berry CN, Giradot C, Lecoffre C, Lunven C: Effects of the synthetic thrombin inhibitor argatroban on fibrin- or clot-incorporated thrombin: comparison with heparin and recombinant hirudin. Thromb Haemost 1994, 72:381-386.
    • (1994) Thromb Haemost , vol.72 , pp. 381-386
    • Berry, C.N.1    Giradot, C.2    Lecoffre, C.3    Lunven, C.4
  • 9
    • 0028292930 scopus 로고
    • Inhibition of factor Xa-induced platelet aggregation by a selective thrombin inhibitor, argatroban
    • Kawai H, Yamamoto T, Hara H, Tamao Y: Inhibition of factor Xa-induced platelet aggregation by a selective thrombin inhibitor, argatroban. Thromb Res 1994, 74:185-191.
    • (1994) Thromb Res , vol.74 , pp. 185-191
    • Kawai, H.1    Yamamoto, T.2    Hara, H.3    Tamao, Y.4
  • 10
    • 0022981986 scopus 로고
    • Effect of argipidine (MD 805) on platelet function
    • Hara H, Tamao Y, Kikumoto R: Effect of argipidine (MD 805) on platelet function. Jpn Pharmacol Ther 1986, 14:13-20.
    • (1986) Jpn Pharmacol Ther , vol.14 , pp. 13-20
    • Hara, H.1    Tamao, Y.2    Kikumoto, R.3
  • 11
    • 0027739273 scopus 로고
    • Heparin inhibits endothelin-1 and protooncogene c-fos gene expression in cultured bovine endothelial cells
    • Imai T, Hirata Y, Marumo F: Heparin inhibits endothelin-1 and protooncogene c-fos gene expression in cultured bovine endothelial cells. J Cardiovasc Pharmacol 1993, 22 (suppl 8):S49-S52.
    • (1993) J Cardiovasc Pharmacol , vol.22 , Issue.8 SUPPL.
    • Imai, T.1    Hirata, Y.2    Marumo, F.3
  • 12
    • 0027360442 scopus 로고
    • Argatroban and inhibition of the vasomotor actions of thrombin
    • Winn MJ, Jain K, Ku DD: Argatroban and inhibition of the vasomotor actions of thrombin. J Cardiovasc Pharmacol 1993, 22:754-760.
    • (1993) J Cardiovasc Pharmacol , vol.22 , pp. 754-760
    • Winn, M.J.1    Jain, K.2    Ku, D.D.3
  • 13
    • 0027368915 scopus 로고    scopus 로고
    • Involvement of the 'tethered ligand' receptor in thrombin-induced endothelium mediated relaxations
    • Tesfamariam B, Allen GT, Normandin D, Antonaccio MJ: Involvement of the 'tethered ligand' receptor in thrombin-induced endothelium mediated relaxations. Am J Physiol 265:H1744-H1749.
    • Am J Physiol , vol.265
    • Tesfamariam, B.1    Allen, G.T.2    Normandin, D.3    Antonaccio, M.J.4
  • 14
    • 0022462370 scopus 로고
    • Effect of a selective thrombin inhibitor MCI-9038 on fibrinolysis in vitro and in vivo
    • Tamao Y, Yamamoto T, Kikumoto R, Hara H, Itoh J, Hirata T, et al.: Effect of a selective thrombin inhibitor MCI-9038 on fibrinolysis in vitro and in vivo. Thromb Haemost 1986, 56:28-34. Careful series of studies to examine whether argatroban inhibited the enzymes involved in clot lysis. Confirmation of studies using purified enzymes demonstrating the thrombin specificity of argatroban
    • (1986) Thromb Haemost , vol.56 , pp. 28-34
    • Tamao, Y.1    Yamamoto, T.2    Kikumoto, R.3    Hara, H.4    Itoh, J.5    Hirata, T.6
  • 16
    • 0025143892 scopus 로고
    • Comparative effects of aspirin, a synthetic thrombin inhibitor and a monoclonal antiplatelet glycoprotein IIb/IIIa antibody on coronary artery reperfusion, reocclusion and bleeding time with recombinant tissue-type plasminogen activator in a canine preparation
    • Yasuda T, Gold HK, Yaoita H, Leinbach RC, Guerrero JL, Jang IK, et al.: Comparative effects of aspirin, a synthetic thrombin inhibitor and a monoclonal antiplatelet glycoprotein IIb/IIIa antibody on coronary artery reperfusion, reocclusion and bleeding time with recombinant tissue-type plasminogen activator in a canine preparation. J Am Coll Cardiol 1990, 16:714-722.
    • (1990) J Am Coll Cardiol , vol.16 , pp. 714-722
    • Yasuda, T.1    Gold, H.K.2    Yaoita, H.3    Leinbach, R.C.4    Guerrero, J.L.5    Jang, I.K.6
  • 17
    • 0028004409 scopus 로고
    • Antithrombotic actions of argatroban in rat models of venous, 'mixed' and arterial thrombosis, and its effects on the tail transection bleeding time
    • Berry CN, Girard D, Lochot S, Lecoffre C: 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 1994, 113:1209-1214.
    • (1994) Br J Pharmacol , vol.113 , pp. 1209-1214
    • Berry, C.N.1    Girard, D.2    Lochot, S.3    Lecoffre, C.4
  • 18
    • 0024411829 scopus 로고
    • Thrombin is an important mediator of platelet aggregation in stenosed canine coronary arteries with endothelial injury
    • Eidt JF, Allison P, Noble S, Ashton J, Golino P, McNatt J, et al.: Thrombin is an important mediator of platelet aggregation in stenosed canine coronary arteries with endothelial injury. J Clin Invest 1989, 84:18-27.
    • (1989) J Clin Invest , vol.84 , pp. 18-27
    • Eidt, J.F.1    Allison, P.2    Noble, S.3    Ashton, J.4    Golino, P.5    McNatt, J.6
  • 19
    • 0025017743 scopus 로고
    • Prevention of platelet-rich thrombosis by selective thrombin inhibition
    • Jang IK, Gold HK, Ziskind AA, Leinbach RC, Fallon JT, Collen D: Prevention of platelet-rich thrombosis by selective thrombin inhibition. Circulation 1990, 81:219-225. First demonstration of the antithrombotic effects of argatroban in a model of coronary thrombosis that is highly platelet-dependent.
    • (1990) Circulation , vol.81 , pp. 219-225
    • Jang, I.K.1    Gold, H.K.2    Ziskind, A.A.3    Leinbach, R.C.4    Fallon, J.T.5    Collen, D.6
  • 20
    • 0019854196 scopus 로고
    • Comparative study of heparin and a synthetic thrombin inhibitor No 805 (MD-805) in experimental antithrombin III-deficient animals
    • Kumada T, Abiko Y: Comparative study of heparin and a synthetic thrombin inhibitor No 805 (MD-805) in experimental antithrombin III-deficient animals. Thromb Res 1981, 24:285-298.
    • (1981) Thromb Res , vol.24 , pp. 285-298
    • Kumada, T.1    Abiko, Y.2
  • 21
    • 0028099887 scopus 로고
    • Enhancement of thrombolytic efficacy of tissue-type plasminogen activator by adjuvants in guinea pig thrombosis model
    • Nishiyama H, Umemura K, Saniabadi AR, Takiguchi AR, Uematsu T, Nakashima M: Enhancement of thrombolytic efficacy of tissue-type plasminogen activator by adjuvants in guinea pig thrombosis model. Eur J Pharmacol 1994, 264:191-198.
    • (1994) Eur J Pharmacol , vol.264 , pp. 191-198
    • Nishiyama, H.1    Umemura, K.2    Saniabadi, A.R.3    Takiguchi, A.R.4    Uematsu, T.5    Nakashima, M.6
  • 22
    • 0025676311 scopus 로고
    • Prevention of reocclusion by MCI-9038, a thrombin inhibitor, following t-PA-induced thrombolysis in a canine model of femoral arterial thrombosis
    • Mellott MJ, Connolly TM, Bush LR: Prevention of reocclusion by MCI-9038, a thrombin inhibitor, following t-PA-induced thrombolysis in a canine model of femoral arterial thrombosis. Thromb Haemost 1990, 64:526-530.
    • (1990) Thromb Haemost , vol.64 , pp. 526-530
    • Mellott, M.J.1    Connolly, T.M.2    Bush, L.R.3
  • 23
    • 0025648376 scopus 로고
    • In vivo thrombin inhibition enhances and sustains arterial recanalization with recombinant tissue-type plasminogen activator
    • Jang IK, Gold HK, Leinbach RC, Fallon JY, Collen D: In vivo thrombin inhibition enhances and sustains arterial recanalization with recombinant tissue-type plasminogen activator. Circ Res 1990, 67:1552-1561.
    • (1990) Circ Res , vol.67 , pp. 1552-1561
    • Jang, I.K.1    Gold, H.K.2    Leinbach, R.C.3    Fallon, J.Y.4    Collen, D.5
  • 24
    • 0025143892 scopus 로고
    • Comparative effects of aspirin, a synthetic thrombin inhibitor and a monoclonal antiplatelet glycoprotein Iib/IIIa antibody on coronary artery reperfusion, reocclusion and bleeding with recombinant tissue-type plasminogen activator in a canine preparation
    • Yasuda T, Gold HK, Yaoita H, Leinbach RC, Guerrero JL, Jang IK, et al.: Comparative effects of aspirin, a synthetic thrombin inhibitor and a monoclonal antiplatelet glycoprotein Iib/IIIa antibody on coronary artery reperfusion, reocclusion and bleeding with recombinant tissue-type plasminogen activator in a canine preparation. J Am Coll Cardiol 1990, 16:714-720.
    • (1990) J Am Coll Cardiol , vol.16 , pp. 714-720
    • Yasuda, T.1    Gold, H.K.2    Yaoita, H.3    Leinbach, R.C.4    Guerrero, J.L.5    Jang, I.K.6
  • 25
    • 0026353329 scopus 로고
    • Heparin and the thrombin inhibitor argatroban enhance fibrinolysis by infused or bolus-injected saruplase in rabbit femoral artery thrombosis
    • Schneider J: Heparin and the thrombin inhibitor argatroban enhance fibrinolysis by infused or bolus-injected saruplase in rabbit femoral artery thrombosis. Thromb Res 1991, 64:677-689.
    • (1991) Thromb Res , vol.64 , pp. 677-689
    • Schneider, J.1
  • 26
    • 0026799510 scopus 로고
    • Synergistic antithrombotic properties of G 4120, a RGD-containing synthetic peptide, and argatroban, a synthetic thrombin inhibitor, in a hamster femoral vein platelet-rich thrombosis model
    • Imura Y, Stassen JM, Vreys I, Lesaffre E, Gold HK, Collen D: Synergistic antithrombotic properties of G 4120, a RGD-containing synthetic peptide, and argatroban, a synthetic thrombin inhibitor, in a hamster femoral vein platelet-rich thrombosis model. Thromb Haemost 1992, 68:336-340. The effects of a thrombin inhibitor may be enhanced by antiplatelet therapy, in this case an antagonist of the platelet glycoprotein IIb/IIIa.
    • (1992) Thromb Haemost , vol.68 , pp. 336-340
    • Imura, Y.1    Stassen, J.M.2    Vreys, I.3    Lesaffre, E.4    Gold, H.K.5    Collen, D.6
  • 28
    • 0025757180 scopus 로고
    • Combined administration of aspirin and a specific thrombin inhibitor in man
    • Clarke RJ, Mayo G, FitzGerald GA, Fitzgerald DJ: Combined administration of aspirin and a specific thrombin inhibitor in man. Circulation 1991, 83:1510-1518.
    • (1991) Circulation , vol.83 , pp. 1510-1518
    • Clarke, R.J.1    Mayo, G.2    FitzGerald, G.A.3    Fitzgerald, D.J.4
  • 30
    • 0027457174 scopus 로고
    • Evidence for a rebound coagulation phenomenon after cessation of a 4-hour infusion of a specific thrombin inhibitor
    • Gold HK, Torres FW, Garabedian HD, Werner W, Jang IK, Khan A, et al.: Evidence for a rebound coagulation phenomenon after cessation of a 4-hour infusion of a specific thrombin inhibitor. J Am Coll Cardiol 1993, 21:1039-1047. First extensive clinical trial of argatroban in patients with unstable angina using escalating doses of the drug. Symptoms recurred after withdrawal of the drug, raising concerns that competitive inhibitors are subject to a rebound phenomenom. However, it is worth noting that aspirin was withheld.
    • (1993) J Am Coll Cardiol , vol.21 , pp. 1039-1047
    • Gold, H.K.1    Torres, F.W.2    Garabedian, H.D.3    Werner, W.4    Jang, I.K.5    Khan, A.6
  • 31
    • 0026736119 scopus 로고
    • Reactivation of unstable angina after the discontinuation of heparin
    • Theroux P, Waters D, Lam J, Juneau M, McCans J: Reactivation of unstable angina after the discontinuation of heparin. N Engl J Med 1992, 327:141-145. A similar rebound is reported on withdrawal of heparin in patients with unstable angina. As heparin inactivates thrombin by accelerating the activity of antithrombin III, the rebound seen with argatroban may reflect the natural history of the disease, which requires days to stabilize.
    • (1992) N Engl J Med , vol.327 , pp. 141-145
    • Theroux, P.1    Waters, D.2    Lam, J.3    Juneau, M.4    McCans, J.5
  • 32
    • 0022652413 scopus 로고
    • Effects of a new anticoagulant (MO 805) on platelet activation in the haemodialysis circuit
    • Matsuo T, Nakao K, Yamada T, Matsuo O: Effects of a new anticoagulant (MO 805) on platelet activation in the haemodialysis circuit. Thromb Res 1986, 41:33-41.
    • (1986) Thromb Res , vol.41 , pp. 33-41
    • Matsuo, T.1    Nakao, K.2    Yamada, T.3    Matsuo, O.4
  • 33
    • 0023709275 scopus 로고
    • Effect of synthetic thrombin inhibitor (MD 805) as an alternative drug on heparin induced thrombocytopenia during hemodialysis
    • Matsuo T, Chikahira Y, Yamada T, Nakao K, Ueshima S, Matsuo O: Effect of synthetic thrombin inhibitor (MD 805) as an alternative drug on heparin induced thrombocytopenia during hemodialysis. Thromb Res 1988, 52:165-171.
    • (1988) Thromb Res , vol.52 , pp. 165-171
    • Matsuo, T.1    Chikahira, Y.2    Yamada, T.3    Nakao, K.4    Ueshima, S.5    Matsuo, O.6


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