The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist properties

British Journal of Pharmacology

Volumn 129, Issue 7, 2000, Pages 1439-1446

  Sugidachi, Atsuhiro ^a   Asai, Fumitoshi ^a   Ogawa, Taketoshi ^a   Inoue, Teruhiko ^b   Koike, Hiroyuki ^a  

^a DAIICHI SANKYO CO   (Japan)

^b UBE INDUSTRIES LTD   (Japan)

Author keywords

Active metabolite; Bleeding time; CS 747; Platelet ADP receptors; Platelet aggregation; R 99224; Thrombosis

Indexed keywords

2 METHYLTHIOADENOSINE TRIPHOSPHATE; ADENOSINE DIPHOSPHATE; ADENOSINE DIPHOSPHATE RECEPTOR; ANTITHROMBOCYTIC AGENT; CELL RECEPTOR; CLOPIDOGREL; CYCLIC AMP; PRASUGREL; PROSTAGLANDIN E1; PURINE P2 RECEPTOR; R 99224; THROMBIN; TICLOPIDINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLEEDING TIME; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG POTENCY; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BLOCKING; THROMBOCYTE AGGREGATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOGENESIS;

EID: 0034068625     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703237     Document Type: Article

References (39)

1. Antiplatelet Trialists' Collaboration. (1988). Secondary prevention of vascular disease by prolonged antiplatelet treatment. Br. Med. J., 296, 320-331.
2. CAPRIE Steering Committee. (1996). A randomized, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE). Lancet, 348, 1329-1339.
3. Cattaneo, M., Winocour, P.D., Somers, D.A., Groves, H.M., Kinlough-Rathbone, R.L., Packham, M.A. & Mustard, J.F. (1985). Effect of ticlopidine on platelet aggregation, adherence to damaged vessels, thrombus formation and platelet survival. Thromb. Res., 37, 29-43.
4. Coukell, A.J. & Markham, A. (1997). Clopidogrel. Drugs, 54, 745-750.
5. Daniel, J.L., Dangelmaier, G., Jin, J., Ashby, B., Smith, J.B. & Kunapuli, S.P. (1998). Molecular basis for ADP-induced platelet activation. I. Evidence for three distinct ADP receptors on human platelets. J. Biol. Chem., 273, 2024-2029.
6. 1-activated platelet adenylyl cyclase in rats and rabbits. Thromb. Haemost., 65, 186-190.
7. Dejana, E., Callioni, A., Quintana, A. & De Gaetano, G. (1979). Bleeding time in laboratory animals. II - A comparison of different assay conditions in rats. Thromb. Res., 15, 191-197.
8. Emms, H. & Lewis, G.P. (1986). The role of prostaglandin endoperoxides, thromboxane A2 and adenosine diphosphate in collagen-induced aggregation in man and the rat. Br. J. Pharmacol., 87, 109-115.
9. Fagura, M.S., Dainty, I.A., McKay, G.D., Kirk, I.P., Humphries, R.G., Robertson, M.J., Dougall, I.G. & Leff, P. (1998). P2Y1-receptors in human platelets which are pharmacologically distinct from P2Y (ADP)-receptors. Br. J. Pharmacol., 124, 157-164.
10. Gachet, C., Cattaneo, M., Ohlmann, P., Hechler, B., Lecchi, A., Chevalier, J., Cassel, D., Mannucci, P.M. & Cazenave, J.P. (1995). Purinoceptors on blood platelets: further pharmacological and clinical evidence to suggest the presence of two ADP receptors. Br. J. Haematol., 91, 434-444.
11. Gachet, C. & Cazenave, J.P. (1991). ADP induced blood platelet activation: a review. Nouv. Rev. Fr. Hematol., 33, 347-358.
12. Gachet, C., Hechler, B., Lèon, C., Vial, C., Ohlmann, P. & Cazenave, J.P. (1996). Purinergic receptors on blood platelets. Platelets, 7, 261-267.
13. Gent, M., Blakely, J.A., Easton, J.D., Ellis, D.J., Hachinski, V.C., Harbison, J.W., Panak, E., Roberts, R.S., Sicurella, J. & Turpie, A.G. (1989). The Canadian American Ticlopidine Study (CATS) in thromboembolic stroke. Lancet, i, 1215-1220.
14. Hass, W.K., Easton, J.D., Adams Jr. H.P., Pryse-Phillips, W., Molony, B.A., Anderson, S. & Kamm, B. (1989). A randomized trial comparing ticlopidine hydrochloride with aspirin for the prevention of stroke in high-risk patients. N. Engl. J. Med., 321, 501-507.
15. Herbert, J.M., Bernat, A., Samama, M. & Maffrand, J.P. (1996). The antiaggregating and antithrombotic activity of ticlopidine is potentiated by aspirin in the rat. Thromb. Haemost., 76, 94-98.
16. Hourani, S.M.O. & Hall, D.A. (1994). Receptors for ADP on human blood platelets. Trends Pharmacol. Sci., 15, 103-108.
17. Jackson, C.W., Steward, S.A., Ashmun, R.A. & McDonald, T.P. (1992). Megakaryocytopoiesis and platelet production are stimulated during late pregnancy and early postpartum in the rat. Blood, 79, 1672-1678.
18. Jantzen, H.-M., Gousset, L., Bhaskar, V., Vincent, D., Tai, A., Reynolds, E.E. & Conley, P.B. (1998). Evidence for two distinct G-protein-coupled ADP receptors mediating platelet activation. Thromb. Haemost., 81, 111-117.
19. Kunapuli, S.P. (1998a). Multiple P2 receptor subtypes on platelets: a new interpretation of their function. Trends Pharmacol. Sci., 19, 391-394.
20. Kunapuli, S.P. (1998b). Functional characterization of platelet ADP receptors. Platelets, 9, 343-351.
21. MacKenzie, A.B., Mahaut-Smith, M.P. & Sage, S.O. (1996). Activation of receptor-operated cation channels via P2X1 not P2T purinoceptors in human platelets. J. Biol. Chem., 271, 2879-2881.
22. Maffrand, J.P., Bernat, A., Delebassee, D., Defreyn, G., Cazenave, J.P. & Gordon, J.L. (1988). ADP plays a key role in thrombogenesis in rats. Thromb. Haemost., 59, 225-230.
23. McTavish, D., Faulds, D. & Goa, K.L. (1990). Ticlopidine. An updated review of its pharmacology and therapeutic use in platelet-dependent disorders. Drugs, 40, 238-259.
24. Michal, E. & Motamed, M. (1976). Shape change and aggregation of blood platelets: interaction between the effects of adenosine diphosphate, 5-hydroxytryptamine and adrenaline. Br. J. Pharmacol., 56, 209-218.
25. Mills, D.C., Puri, R., Hu, C.J., Minniti, C., Grana, G., Freedman, M.D., Colman, R.F. & Colman, R.W. (1992). Clopidogrel inhibits the binding of ADP analogues to the receptor mediating inhibition of platelet adenylate cyclase. Arterioscler. Thromb., 12, 430-436.
26. Odawara, A., Kikkawa, K., Katoh, M., Toryu, H., Shimazaki, T. & Sasaki, Y. (1996). Inhibitory effects of TA-993, a new 1,5-benzothiazepine derivative, on platelet aggregation. Circ. Res., 78, 643-649.
27. Ohlmann, P., Laugwitz, K.L., Nurnberg, B., Spicher, K., Schultz, G., Cazenave, J.P. & Gachet, C. (1995). The human platelet ADP receptor activates Gi2 proteins. Biochem. J., 312, 775-779.
28. Saltiel, E. & Ward, A. (1987). Ticlopidine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in platelet-dependent disease states. Drugs, 34, 222-262.
29. Savi, P., Combalbert, J., Gaich, C., Rouchon, M.C., Maffrand, J.P., Berger, Y. & Herbert, J.M. (1994b). The antiaggregating activity of clopidogrel is due to a metabolic activation by the hepatic cytochrome P450-1A. Thromb. Haemost., 72, 313-317.
30. Savi, P., Herbert, J.M., Pflieger, A.M., Dol, F., Delebassee, D., Combalbert, J., Defreyn, G. & Maffrand, J.P. (1992). Importance of hepatic metabolism in the antiaggregating activity of the thienopyridine clopidogrel. Biochem. Pharmacol., 44, 527-532.
31. 3H]-2-methylthio ADP to rat platelets-effect of clopidogrel and ticlopidine. J. Pharmacol. Exp. Ther., 269, 772-777.
32. Savi, P., Pflieger, A.M. & Herbert, J.M. (1996). cAMP is not an important messenger for ADP-induced platelet aggregation. Blood Coagul. Fibrinolysis, 7, 249-252.
33. Schrör, K. (1995). Antiplatelet drugs. Drugs, 50, 7-28.
34. Sugidachi, A., Asai, F. & Koike, H. (1993). In vivo pharmacology of aprosulate, a new synthetic polyanion with anticoagulant activity. Thromb. Res., 69, 71-80.
35. Sugidachi, A., Ogawa, T., Asai, F., Saito, S., Ozaki, H., Fusetani, N., Karaki, H & Koike, H. (1998). Inhibition of rat platelet aggregation by mycalolide-B, a novel inhibitor of actin polymerization with a different mechanism of action from cytochalasin-D. Thromb. Haemost., 79, 614-619.
36. Tschopp, T.B. & Zucker, M.B. (1972). Hereditary defect in platelet function in rats. Blood, 40, 217-266.
37. Umetsu, T. & Sanai, K. (1978). Effect of 1-methyl-2-mercapto-5-(3-pyridyl)-imidazole (KC-6141), an anti-aggregating compound, on experimental thrombosis in rats. Thromb. Haemost., 39, 74-83.
38. Weber, A.A., Reimann, S. & Schrör, K. (1999). Specific inhibition of ADP-induced platelet aggregation by clopidogrel in vitro. Br. J. Pharmacol., 126, 415-420.
39. Wey, H., Gallon, L. & Subbiah, M.T.R. (1982). Prostaglandin synthesis in aorta and platelets of fawn-hooded rats with platelet storage pool disease and its response to cholesterol feeding. Thromb. Haemostas., 48, 94-97.