Effects of a new PAR1 antagonist, F 16618, on smooth muscle cell contraction

European Journal of Pharmacology

Volumn 611, Issue 1-3, 2009, Pages 60-63

  Bocquet, Arnaud ^a   Létienne, Robert ^a   Sablayrolles, Sylvie ^a   De Vries, Luc ^a   Perez, Michel ^a   Le Grand, Bruno ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

PAR1 antagonist; Vasoconstriction; Vessel

Indexed keywords

CALCIUM; ER 121958; F 16618; PROTEINASE ACTIVATED RECEPTOR 1; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD VESSEL INJURY; BLOOD VESSEL TONE; CALCIUM TRANSPORT; CHO CELL; COMPETITIVE INHIBITION; CONTROLLED STUDY; CORONARY ARTERY; DRUG EFFECT; FLUORESCENCE; HEART RATE; HEMODYNAMIC PARAMETERS; IC 50; MALE; MEAN ARTERIAL PRESSURE; NONHUMAN; PRIORITY JOURNAL; RAT; SMOOTH MUSCLE CONTRACTION; SUPERIOR MESENTERIC ARTERY; SWINE; VASOSPASM;

ANESTHESIA; ANIMALS; CALCIUM; CHO CELLS; CORONARY VESSELS; CRICETINAE; CRICETULUS; FLUORESCENCE; HEMODYNAMICS; ISOMETRIC CONTRACTION; MALE; MESENTERIC ARTERY, SUPERIOR; MUSCLE CONTRACTION; MYOCYTES, SMOOTH MUSCLE; OLIGOPEPTIDES; PIPERAZINES; PYRIDINES; RATS; RECEPTOR, PAR-1; REFERENCE STANDARDS; SWINE;

EID: 67349088403     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.03.056     Document Type: Article

References (16)

1. Andrade-Gordon P., Derian C.K., Maryanoff B.E., Zhang H.C., Addo M.F., Cheung W.M., Damiano B.P., D'Andrea M.R., Darrow A.L., de Garavilla L., Eckardt A.J., Giardino B.C., Haertlein B.J., and McComsey D.F. 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 (2001) 34-42
2. Fukunaga R., Hirano K., Hirano M., Niiro N., Nishimura J., Maehara Y., and Kanaide H. Upregulation of proteinase-activated receptors and hypercontractile responses precede development of arterial lesions after balloon injury. Am. J. Physiol. Heart Circ. Physiol. 291 (2006) H2388-2395
3. Hamilton J.R., and Cocks T.M. Heterogeneous mechanisms of endothelium-dependent relaxation for thrombin and peptide activators of protease-activated receptor-1 in porcine isolated coronary artery. Br. J. Pharmacol. 130 (2000) 181-188
4. Hatton M.W., Moar S.L., and Richardson M. Deendothelialization in vivo initiates a thrombogenic reaction at the rabbit aorta surface. Correlation of uptake of fibrinogen and antithrombin III with thrombin generation by the exposed subendothelium. Am. J. Pathol. 135 (1989) 499-508
5. Hirano K., Yufu T., Hirano M., Nishimura J., and Kanaide H. Physiology and pathophysiology of proteinase-activated receptors (PARs): regulation of the expression of PARs. J. Pharmacol. Sci. 97 (2005) 31-37
6. Kai Y., Hirano K., Maeda Y., Nishimura J., Sasaki T., and Kanaide H. Prevention of the hypercontractile response to thrombin by proteinase-activated receptor-1 antagonist in subarachnoid hemorrhage. Stroke 38 (2007) 3259-3265
7. Kawabata A., Kubo S., Nakaya Y., Ishiki T., Kuroda R., Sekiguchi F., Kawao N., and Nishikawa H. Distinct roles for protease-activated receptors 1 and 2 in vasomotor modulation in rat superior mesenteric artery. Cardiovasc. Res. 61 (2004) 683-692
8. Ku D.D., and Dai J. Expression of thrombin receptors in human atherosclerotic coronary arteries leads to an exaggerated vasoconstrictory response in vitro. J. Cardiovasc. Pharmacol. 30 (1997) 649-657
9. Ku D.D., and Zaleski J.K. Receptor mechanism of thrombin-induced endothelium-dependent and endothelium-independent coronary vascular effects in dogs. J. Cardiovasc. Pharmacol. 22 (1993) 609-616
10. Macfarlane S.R., Seatter M.J., Kanke T., Hunter G.D., and Plevin R. Proteinase-activated receptors. Pharmacol. Rev. 53 (2001) 245-282
11. Maeda Y., Hirano K., Kai Y., Hirano M., Suzuki S.O., Sasaki T., and Kanaide H. Up-regulation of proteinase-activated receptor 1 and increased contractile responses to thrombin after subarachnoid haemorrhage. Br. J. Pharmacol. 152 (2007) 1131-1139
12. Mizuno O., Hirano K., Nishimura J., Kubo C., and Kanaide H. Mechanism of endothelium-dependent relaxation induced by thrombin in the pig coronary artery. Eur. J. Pharmacol. 351 (1998) 67-77
13. Nelken N.A., Soifer S.J., O'Keefe J., Vu T.K., Charo I.F., and Coughlin S.R. Thrombin receptor expression in normal and atherosclerotic human arteries. J. Clin. Invest. 90 (1992) 1614-1621
14. Pauwels P.J., and Colpaert F.C. Partial to complete antagonism by putative antagonists at the wild-type alpha (2C)-adrenoceptor based on kinetic analyses of agonist: antagonist interactions. Br J Pharmacol. 131 (2000) 1385-1390
15. Takada M., Tanaka H., Yamada T., Ito O., Kogushi M., Yanagimachi M., Kawamura T., Musha T., Yoshida F., Ito M., Kobayashi H., Yoshitake S., and Saito I. Antibody to thrombin receptor inhibits neointimal smooth muscle cell accumulation without causing inhibition of platelet aggregation or altering hemostatic parameters after angioplasty in rat. Circ. Res. 82 (1998) 980-987
16. Vu T.K., Hung D.T., Wheaton V.I., and Coughlin S.R. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell 64 (1991) 1057-1068