Antiplatelet activity of [5-(2-methoxy-5-chlorophenyl)furan-2-ylcarbonyl] guanidine (KR-32570), a novel sodium/hydrogen exchanger-1 and its mechanism of action

Archives of Pharmacal Research

Volumn 29, Issue 5, 2006, Pages 375-383

  Lee, Kyung Sup ^a   Park, Jung Woo ^b   Jin, Yong Ri ^a   Jung, In Sang ^b   Cho, Mi Ra ^a   Yi, Kyu Yang ^c   Yoo, Sung Eun ^c   Chung, Hun Jong ^b   Yun, Yeo Pyo ^a   Park, Tae Kyu ^b   Shin, Hwa Sup ^b  

^a Chungbuk National University   (South Korea)

^b Konkuk University   (South Korea)

^c Korea Research Institute of Chemical Technology   (South Korea)

Author keywords

KR 32570; NHE 1; Platelet; Platelet swelling test; Washed rabbit platelet

Indexed keywords

(5 (2 METHOXY 5 CHLORO 5 PHENYL)FURAN 2 YLCARBONYL)GUANIDINE; (5-(2-METHOXY-5-CHLORO-5-PHENYL)FURAN-2-YLCARBONYL)GUANIDINE; ANTITHROMBOCYTIC AGENT; ARACHIDONIC ACID; CALCIUM; COLLAGEN; GROWTH FACTOR ACTIVATABLE NA H EXCHANGER NHE 1; GROWTH FACTOR-ACTIVATABLE NA-H EXCHANGER NHE-1; GUANIDINE DERIVATIVE; SEROTONIN; SODIUM PROTON EXCHANGE PROTEIN; THROMBOXANE B2; THROMBOXANE SYNTHASE;

ANIMAL; ARTICLE; DOSE RESPONSE; DRUG ANTAGONISM; DRUG EFFECT; IN VITRO STUDY; METABOLISM; RABBIT; THROMBOCYTE AGGREGATION;

ANIMALS; ARACHIDONIC ACID; CALCIUM; COLLAGEN; DOSE-RESPONSE RELATIONSHIP, DRUG; GUANIDINES; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; RABBITS; SEROTONIN; SODIUM-HYDROGEN ANTIPORTER; THROMBOXANE B2; THROMBOXANE-A SYNTHASE;

EID: 33744941584     PISSN: 02536269     EISSN: 02536269     Source Type: Journal    
DOI: 10.1007/BF02968587     Document Type: Article

References (28)

1. Balsinde, J., Winstead, M. V., and Dennis, E. A., Phospholipase A(2) regulation of arachidonic acid mobilization. FEBS Lett., 531, 2-6 (2002).
2. Born, G. V. and Cross, M. J., The aggregation of blood platelets. J. Physiol., 168, 178-195 (1963).
3. Corti, R., Farkouh, M. E., and Badimon, J. J., The vulnerable plaque, acute coronary syndromes. Am. J. Med., 113, 668-680 (2002).
4. Corti, R., Fuster, V., and Badimon, J. J., Pathogenetic concepts of acute coronary syndromes. J. Am. Coll. Cardiol., 41, 7S-14S (2003).
5. Drayer, A. L., Meima, M. E., Derks, M. W., Tuik, R., and van Haastert, P. J., Mutation of an EF-hand Ca(2+)-binding motif in phospholipase C of Dictyostelium discoideum: inhibition of activity but no effect on Ca2+-dependence. Biochem. J., 311, 505-510 (1995).
6. Holmsen, H. and Dangelmarier, C. A., Measurement of secretion of serotonin. Methods Enzymol., 169, 205-210 (1989).
7. Jackson, S. P., Nesbitt, W. S., and Kulkarni, S., Signaling events underlying thrombus formation. J. Thromb. Haemost., 1, 1602-1612 (2003).
8. 2+ mobilization. J. Pharmacol. Exp. Ther., 312, 214-219 (2005).
9. Jneid, H., Bhatt, D. L., Corti, R., Badimon, J. J., Fuster, V., and Francis, G. S., Aspirin, clopidogrel in acute coronary syndromes: therapeutic insights from the CURE study. Arch. Intern. Med., 163, 1145-1153 (2003).
10. Karmazyn, M., Gan, X. T., Humphreys, R. A., Yoshida, H., and Kusumoto, K., The myocardial Na+-H+ exchange: structure, regulation, its role in heart disease. Circ. Res., 85, 777-786 (1999).
11. Karmazyn, M., Role of sodium-hydrogen exchange in cardiac hypertrophy, heart failure: a novel, promising therapeutic target. Basic. Res. Cardiol., 96, 325-328 (2001).
12. Klages, B., Brandt, U., Simon, M. I., Schultz, G., and Offermanns, S., Activation of G12/G13 results in shape change, Rho/Rho-kinase-mediated myosin light chain phosphorylation in mouse platelets. J. Cell. Biol., 144, 745-754 (1999).
13. Knight, D. R., Smith, A. H., Flynn, D. M., MacAndrew, J. T., Ellery, S. S., Kong, J. X., Marala, R. B., Wester, R. T., Guzman-Perez, A., Hill, R. J., Magee, W. P., and Tracey, W. R., A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reduces ischemic myocardial injury in vitro and in vivo. J. Pharmacol. Exp. Ther., 297(1), 254-259 (2001).
14. + exchange inhibitor, T-162559. Br. J. Pharmacol., 135(8), 1995-2003 (2002).
15. Lapetina, E. G., The signal transduction induced by thrombin in human platelets. FEBS Lett., 268, 400-404 (1990).
16. Marala, R. B., Brown, J. A., Kong, J. X., Tracey, W. R., Knight, D. R., Wester, R. T., Sun, D., Kennedy, S. P., Hamanaka, E. S., Ruggeri, R. B., and Hill, R. J., Zoniporide: a potent and highly selective inhibitor of human Na+/H+ exchanger-1. Eur. J. Pharmacol., 451(1), 37-41 (2002).
17. Mentzer, R. M. Jr, Lasley, R. D., Jessel, A., and Karmazyn, M., Intracellular sodium hydrogen exchange inhibition, clinical myocardial protection. Ann. Thorac. Surg., 75, S700-S708 (2003).
18. Offermanns, S., Laugwitz, K. L., Spicher, K., and Schultz, G., G proteins of the G12 family are activated via thromboxane A2, thrombin receptors in human platelets. Proc. Natl. Acad. Sci., 91, 504-508 (1994).
19. Raychowdhury, M. K., Yukawa, M., Collins, L. J., McGrail, S. H., Kent, K. C., and Ware, J. A., Alternative splicing produces a divergent cytoplasmic tail in the human endothelial thromboxane A2 receptor. J. Biol. Chem., 269, 19256-19261 (1994).
20. Roberts, D. E., McNicol, A., and Bose, R., Mechanism of collagen activation in human platelets. J. Biol. Chem., 279, 19421-19430 (2004).
21. Rosskopf, D., Sodium-hydrogen exchange, platelet function. J. Thromb. Thrombolysis., 8, 15-24 (1999).
22. + exchange in platelets of patients with essential hypertension using an optical swelling assay. J. Hypertens., 9(3), 231-238 (1991).
23. Ruiz-Meana, M., Garcia-Dorado, D., Pina, P., Inserte, J., Agullo, L., and Soler-Soler, J., Cariporide preserves mitochondrial proton gradient, delays ATP depletion in cardiomyocytes during ischemic conditions. Am. J. Physiol. Heart. Circ. Physiol., 285, H999-1006 (2003).
24. Schlienger, R. G. and Meier, C. R., Effect of selective serotonin reuptake inhibitors on platelet activation: can they prevent acute myocardial infarction? Am. J. Cardiovasc. Drugs., 3, 149-162 (2003).
25. Siffert, W., Regulation of platelet function by sodium-hydrogen exchange. Cardiovasc. Res., 29, 160-166 (1995).
26. + exchanger in the formation of microvesicles by porcine platelets. Haematologia (Budap), 32, 239-252 (2002).
27. The RAPT Investigators, Randomized trial of ridogrel, a combined thromboxane A2 synthase inhibitor, thromboxane A2/prostaglandin endoperoxide receptor antagonist, versus aspirin as adjunct to thrombolysis in patients with acute myocardial infarction. The Ridogrel Versus Aspirin Patency Trial (RAPT). Circulation, 89, 588-595 (1994).
28. Touret, N., Tanneur, V., Godart, H., Seidler, R., Taki, N., and Burger, E., et al. Characterization of sabiporide, a new specific NHE-1 inhibitor exhibiting slow dissociation kinetics, cardioprotective effects. Eur. J. Pharmacol., 459, 151-158 (2003).