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Volumn 165, Issue 6, 2012, Pages 1827-1835

Antiplatelet and antithrombotic effect of F 16618, a new thrombin proteinase-activated receptor-1 (PAR1) antagonist

Author keywords

aggregation; antiplatelet agent; arterial thrombosis; PAR1 antagonist; platelets

Indexed keywords

2 [5 OXO 5 (4 PYRIDIN 2 YL PIPERAZIN 1 YL)PENTA1,3 DIENYL]BENZONITRILE; ANTICOAGULANT AGENT; ANTITHROMBOCYTIC AGENT; COLLAGEN; NEW DRUG; PADGEM PROTEIN; PROTEINASE ACTIVATED RECEPTOR 4; THROMBIN; THROMBIN RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

EID: 84857465754     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01668.x     Document Type: Article
Times cited : (13)

References (37)
  • 1
    • 0034670162 scopus 로고    scopus 로고
    • Inhibition of cellular action of thrombin by N3-cyclopropyl-7-[[4-(1- methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist
    • Ahn HS, Foster C, Boykow G, Stamford A, Manna M, Graziano M, (2000). Inhibition of cellular action of thrombin by N3-cyclopropyl-7-[[4-(1- methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem Pharmacol 60: 1425-1434.
    • (2000) Biochem Pharmacol , vol.60 , pp. 1425-1434
    • Ahn, H.S.1    Foster, C.2    Boykow, G.3    Stamford, A.4    Manna, M.5    Graziano, M.6
  • 2
    • 81355156238 scopus 로고    scopus 로고
    • Guide to Receptors and Channels (GRAC), 5th Edition
    • Alexander SPH, Mathie A, Peters JA, (2011). Guide to Receptors and Channels (GRAC), 5th Edition. Br J Pharmacol 164 (Suppl. 1): S1-S324.
    • (2011) Br J Pharmacol , vol.164 , Issue.SUPPL. 1
    • Alexander, S.P.H.1    Mathie, A.2    Peters, J.A.3
  • 3
    • 0033613269 scopus 로고    scopus 로고
    • Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity
    • Andersen H, Greenberg DL, Fujikawa K, Xu W, Chung DW, Davie EW, (1999). Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci USA 96: 11189-11193.
    • (1999) Proc Natl Acad Sci USA , vol.96 , pp. 11189-11193
    • Andersen, H.1    Greenberg, D.L.2    Fujikawa, K.3    Xu, W.4    Chung, D.W.5    Davie, E.W.6
  • 4
    • 0034967927 scopus 로고    scopus 로고
    • Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats
    • Andrade-Gordon P, Derian CK, Maryanoff BE, Zhang HC, Addo MF, Cheung W, et al,. (2001). Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats. J Pharmacol Exp Ther 298: 34-42.
    • (2001) J Pharmacol Exp Ther , vol.298 , pp. 34-42
    • Andrade-Gordon, P.1    Derian, C.K.2    Maryanoff, B.E.3    Zhang, H.C.4    Addo, M.F.5    Cheung, W.6
  • 7
    • 44949114152 scopus 로고    scopus 로고
    • Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity
    • Chackalamannil S, Wang Y, Greenlee WJ, Hu Z, Xia Y, Ahn HS, (2008). Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem 51: 3061-3064.
    • (2008) J Med Chem , vol.51 , pp. 3061-3064
    • Chackalamannil, S.1    Wang, Y.2    Greenlee, W.J.3    Hu, Z.4    Xia, Y.5    Ahn, H.S.6
  • 8
    • 79951963196 scopus 로고    scopus 로고
    • Protease activated Receptor-1 antagonist, F 16618 reduces arterial restenosis by down-regulation of TNF{alpha} and MMP7 expression, and migration and proliferation of vascular smooth muscle cells
    • Chieng-Yane P, Bocquet A, Letienne R, Bourbon T, Sablayrolles S, Perez M, et al,. (2011). Protease activated Receptor-1 antagonist, F 16618 reduces arterial restenosis by down-regulation of TNF{alpha} and MMP7 expression, and migration and proliferation of vascular smooth muscle cells. J Pharmacol Exp Ther 336: 643-651.
    • (2011) J Pharmacol Exp Ther , vol.336 , pp. 643-651
    • Chieng-Yane, P.1    Bocquet, A.2    Letienne, R.3    Bourbon, T.4    Sablayrolles, S.5    Perez, M.6
  • 9
    • 0036194522 scopus 로고    scopus 로고
    • Mechanisms of action of proteinase-activated receptor agonists on human platelets
    • Chung AW, Jurasz P, Hollenberg MD, Radomski MW, (2002). Mechanisms of action of proteinase-activated receptor agonists on human platelets. Br J Pharmacol 135: 1123-1132.
    • (2002) Br J Pharmacol , vol.135 , pp. 1123-1132
    • Chung, A.W.1    Jurasz, P.2    Hollenberg, M.D.3    Radomski, M.W.4
  • 10
    • 28344436780 scopus 로고    scopus 로고
    • Protease-activated receptors in hemostasis, thrombosis and vascular biology
    • Coughlin SR, (2005). Protease-activated receptors in hemostasis, thrombosis and vascular biology. J Thromb Haemost 3: 1800-1814.
    • (2005) J Thromb Haemost , vol.3 , pp. 1800-1814
    • Coughlin, S.R.1
  • 11
    • 0034625055 scopus 로고    scopus 로고
    • Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets
    • Covic L, Gresser AL, Kuliopulos A, (2000). Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets. Biochemistry 39: 5458-5467.
    • (2000) Biochemistry , vol.39 , pp. 5458-5467
    • Covic, L.1    Gresser, A.L.2    Kuliopulos, A.3
  • 13
    • 0037310962 scopus 로고    scopus 로고
    • Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates
    • Derian CK, Damiano BP, Addo MF, Darrow AL, D'Andrea MR, Nedelman M, et al,. (2003). Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates. J Pharmacol Exp Ther 304: 855-861.
    • (2003) J Pharmacol Exp Ther , vol.304 , pp. 855-861
    • Derian, C.K.1    Damiano, B.P.2    Addo, M.F.3    Darrow, A.L.4    D'Andrea, M.R.5    Nedelman, M.6
  • 15
    • 2142651737 scopus 로고    scopus 로고
    • Role of protease-activated receptors in the vascular system
    • Hirano K, Kanaide H, (2003). Role of protease-activated receptors in the vascular system. J Atheroscler Thromb 10: 211-225.
    • (2003) J Atheroscler Thromb , vol.10 , pp. 211-225
    • Hirano, K.1    Kanaide, H.2
  • 16
    • 58649085872 scopus 로고    scopus 로고
    • Role of platelets in atherothrombosis
    • Jennings LK, (2009). Role of platelets in atherothrombosis. Am J Cardiol 103: 4A-10A.
    • (2009) Am J Cardiol , vol.103
    • Jennings, L.K.1
  • 17
  • 18
    • 0033404539 scopus 로고    scopus 로고
    • In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist
    • Kato Y, Kita Y, Nishio M, Hirasawa Y, Ito K, Yamanaka T, et al,. (1999). In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur J Pharmacol 384: 197-202.
    • (1999) Eur J Pharmacol , vol.384 , pp. 197-202
    • Kato, Y.1    Kita, Y.2    Nishio, M.3    Hirasawa, Y.4    Ito, K.5    Yamanaka, T.6
  • 19
    • 12444304462 scopus 로고    scopus 로고
    • Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig
    • Kato Y, Kita Y, Hirasawa-Taniyama Y, Nishio M, Mihara K, Ito K, et al,. (2003). Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig. Eur J Pharmacol 473: 163-169.
    • (2003) Eur J Pharmacol , vol.473 , pp. 163-169
    • Kato, Y.1    Kita, Y.2    Hirasawa-Taniyama, Y.3    Nishio, M.4    Mihara, K.5    Ito, K.6
  • 20
    • 79952487685 scopus 로고    scopus 로고
    • The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs
    • Kogushi M, Matsuoka T, Kawata T, Kuramochi H, Kawaguchi S, Murakami K, et al,. (2011). The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur J Pharmacol 657: 131-137.
    • (2011) Eur J Pharmacol , vol.657 , pp. 131-137
    • Kogushi, M.1    Matsuoka, T.2    Kawata, T.3    Kuramochi, H.4    Kawaguchi, S.5    Murakami, K.6
  • 21
    • 77950068790 scopus 로고    scopus 로고
    • Antithrombotic activity of F 16618, a new PAR1 antagonist evaluated in extracorporeal arterio-venous shunt in the rat
    • Letienne R, Leparq-Panissie A, Calmettes Y, Nadal-Wollbold F, Perez M, Le Grand B, (2010). Antithrombotic activity of F 16618, a new PAR1 antagonist evaluated in extracorporeal arterio-venous shunt in the rat. Biochem Pharmacol 79: 1616-1621.
    • (2010) Biochem Pharmacol , vol.79 , pp. 1616-1621
    • Letienne, R.1    Leparq-Panissie, A.2    Calmettes, Y.3    Nadal-Wollbold, F.4    Perez, M.5    Le Grand, B.6
  • 22
    • 59849120163 scopus 로고    scopus 로고
    • Cardiovascular death and nonfatal myocardial infarction in acute coronary syndrome patients receiving coronary stenting are predicted by residual platelet reactivity to ADP detected by a point-of-care assay: A 12-month follow-up
    • Marcucci R, Gori AM, Paniccia R, Giusti B, Valente S, Giglioli C, et al,. (2009). Cardiovascular death and nonfatal myocardial infarction in acute coronary syndrome patients receiving coronary stenting are predicted by residual platelet reactivity to ADP detected by a point-of-care assay: a 12-month follow-up. Circulation 119: 237-242.
    • (2009) Circulation , vol.119 , pp. 237-242
    • Marcucci, R.1    Gori, A.M.2    Paniccia, R.3    Giusti, B.4    Valente, S.5    Giglioli, C.6
  • 23
    • 68949156886 scopus 로고    scopus 로고
    • Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: Design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2 degrees P)-TIMI 50 trial
    • Morrow DA, Scirica BM, Fox KA, Berman G, Strony J, Veltri E, et al,. (2009). Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2 degrees P)-TIMI 50 trial. Am Heart J 158: 335-341.
    • (2009) Am Heart J , vol.158 , pp. 335-341
    • Morrow, D.A.1    Scirica, B.M.2    Fox, K.A.3    Berman, G.4    Strony, J.5    Veltri, E.6
  • 24
    • 69549133824 scopus 로고    scopus 로고
    • SCH-530348, a thrombin receptor (PAR-1) antagonist for the prevention and treatment of atherothrombosis
    • Oestreich J, (2009). SCH-530348, a thrombin receptor (PAR-1) antagonist for the prevention and treatment of atherothrombosis. Curr Opin Investig Drugs 10: 988-996.
    • (2009) Curr Opin Investig Drugs , vol.10 , pp. 988-996
    • Oestreich, J.1
  • 25
    • 70349640055 scopus 로고    scopus 로고
    • Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo
    • Perez M, Lamothe M, Maraval C, Mirabel E, Loubat C, Planty B, et al,. (2009). Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo. J Med Chem 52: 5826-5836.
    • (2009) J Med Chem , vol.52 , pp. 5826-5836
    • Perez, M.1    Lamothe, M.2    Maraval, C.3    Mirabel, E.4    Loubat, C.5    Planty, B.6
  • 26
    • 40349085619 scopus 로고    scopus 로고
    • Proteinases and signalling: Pathophysiological and therapeutic implications via PARs and more
    • Ramachandran R, Hollenberg MD, (2008). Proteinases and signalling: pathophysiological and therapeutic implications via PARs and more. Br J Pharmacol 153 (Suppl. 1): S263-S282.
    • (2008) Br J Pharmacol , vol.153 , Issue.SUPPL. 1
    • Ramachandran, R.1    Hollenberg, M.D.2
  • 27
    • 67749086022 scopus 로고    scopus 로고
    • The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease
    • Serebruany VL, Kogushi M, Dastros-Pitei D, Flather M, Bhatt DL, (2009). The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease. Thromb Haemost 102: 111-119.
    • (2009) Thromb Haemost , vol.102 , pp. 111-119
    • Serebruany, V.L.1    Kogushi, M.2    Dastros-Pitei, D.3    Flather, M.4    Bhatt, D.L.5
  • 28
    • 0034682810 scopus 로고    scopus 로고
    • Protease-activated receptors 1 and 4 are shut off with distinct kinetics after activation by thrombin
    • Shapiro MJ, Weiss EJ, Faruqi TR, Coughlin SR, (2000). Protease-activated receptors 1 and 4 are shut off with distinct kinetics after activation by thrombin. J Biol Chem 275: 25216-25221.
    • (2000) J Biol Chem , vol.275 , pp. 25216-25221
    • Shapiro, M.J.1    Weiss, E.J.2    Faruqi, T.R.3    Coughlin, S.R.4
  • 29
    • 70350464420 scopus 로고    scopus 로고
    • Cross validation of the Multiple Electrode Aggregometry. A prospective trial in healthy volunteers
    • Siller-Matula JM, Gouya G, Wolzt M, Jilma B, (2009). Cross validation of the Multiple Electrode Aggregometry. A prospective trial in healthy volunteers. Thromb Haemost 102: 397-403.
    • (2009) Thromb Haemost , vol.102 , pp. 397-403
    • Siller-Matula, J.M.1    Gouya, G.2    Wolzt, M.3    Jilma, B.4
  • 31
    • 34447576539 scopus 로고    scopus 로고
    • Clopidogrel nonresponsiveness in patients undergoing percutaneous coronary intervention with stenting: A systematic review and meta-analysis
    • Snoep JD, Hovens MM, Eikenboom JC, van der Bom JG, Jukema JW, Huisman MV, (2007). Clopidogrel nonresponsiveness in patients undergoing percutaneous coronary intervention with stenting: a systematic review and meta-analysis. Am Heart J 154: 221-231.
    • (2007) Am Heart J , vol.154 , pp. 221-231
    • Snoep, J.D.1    Hovens, M.M.2    Eikenboom, J.C.3    Van Der Bom, J.G.4    Jukema, J.W.5    Huisman, M.V.6
  • 32
    • 33846095378 scopus 로고    scopus 로고
    • Par4 is required for platelet thrombus propagation but not fibrin generation in a mouse model of thrombosis
    • Vandendries ER, Hamilton JR, Coughlin SR, Furie B, Furie BC, (2007). Par4 is required for platelet thrombus propagation but not fibrin generation in a mouse model of thrombosis. Proc Natl Acad Sci USA 104: 288-292.
    • (2007) Proc Natl Acad Sci USA , vol.104 , pp. 288-292
    • Vandendries, E.R.1    Hamilton, J.R.2    Coughlin, S.R.3    Furie, B.4    Furie, B.C.5
  • 33
    • 0026775223 scopus 로고
    • Structure-function relationships in the activation of platelet thrombin receptors by receptor-derived peptides
    • Vassallo RR, Kieber-Emmons T, Cichowski K, Brass LF, (1992). Structure-function relationships in the activation of platelet thrombin receptors by receptor-derived peptides. J Biol Chem 267: 6081-6085.
    • (1992) J Biol Chem , vol.267 , pp. 6081-6085
    • Vassallo, R.R.1    Kieber-Emmons, T.2    Cichowski, K.3    Brass, L.F.4
  • 36
    • 33748307543 scopus 로고    scopus 로고
    • Comparison of the effects of PAR1 antagonists, PAR4 antagonists, and their combinations on thrombin-induced human platelet activation
    • Wu CC, Teng CM, (2006). Comparison of the effects of PAR1 antagonists, PAR4 antagonists, and their combinations on thrombin-induced human platelet activation. Eur J Pharmacol 546: 142-147.
    • (2006) Eur J Pharmacol , vol.546 , pp. 142-147
    • Wu, C.C.1    Teng, C.M.2
  • 37
    • 77956327249 scopus 로고    scopus 로고
    • The roles and mechanisms of PAR4 and P2Y12/phosphatidylinositol 3-kinase pathway in maintaining thrombin-induced platelet aggregation
    • Wu CC, Wu SY, Liao CY, Teng CM, Wu YC, Kuo SC, (2010). The roles and mechanisms of PAR4 and P2Y12/phosphatidylinositol 3-kinase pathway in maintaining thrombin-induced platelet aggregation. Br J Pharmacol 161: 643-658.
    • (2010) Br J Pharmacol , vol.161 , pp. 643-658
    • Wu, C.C.1    Wu, S.Y.2    Liao, C.Y.3    Teng, C.M.4    Wu, Y.C.5    Kuo, S.C.6


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