[en] The sensitivity of bovine platelet aggregation in response to PAF stimulation and the ability of WEB 2086 (a thieno-triazolodiazepine) to inhibit response to PAF-induced platelet aggregation were investigated in the blood from five healthy male Belgian Blue calves. The recorded response to PAF showed a plateau which was dependent on the PAF concentration. Platelet aggregation induced by PAF consists of two mechanisms: reversible and irreversible aggregations which are accompanied by the release of platelet granule contents. Reversible aggregation occurred above (2 . 10(-9) mol/l) PAF, and irreversible aggregation occurred above (2 . 10(-7) mol/l) PAF. Addition of WEB 2086 to bovine platelets in vitro induced a rightward shift in the dose-response curve to PAF. WEB 2086 inhibited PAF-induced aggregation in a competitive reversible manner (pA2 = 7.61). The results of our study show that PAF induces platelet aggregation in platelet-rich plasma (PRP) and that addition of WEB 2086 to bovine platelets in vitro inhibits PAF-induced Platelet Aggregation.
Disciplines :
Anatomy (cytology, histology, embryology...) & physiology Veterinary medicine & animal health
Author, co-author :
Bastos da Silva, Miriam; Université de Liège - ULiège > Faculty of Veterinary Medicine > Laboratory for Functional Investigation
Herion, Francine ; Centre Hospitalier Universitaire de Liège - CHU > Thrombosis Hemostasis Unit
Raskinet, Renée ; Centre Hospitalier Universitaire de Liège - CHU > Thrombosis Hemostasis Unit
David, Jean-Louis ; Université de Liège - ULiège > Thrombosis Hemostasis Unit
Gustin, Pascal ; Université de Liège - ULiège > Pharmacology and Toxicology
Dessy, Cécile ; Université de Liège - ULiège > Faculty of Veterinary Medicine > Histology
Lekeux, Pierre ; Université de Liège - ULiège > Faculty of Veterinary Medicine > Laboratory for Functional Investigation
Language :
English
Title :
Inhibition of Paf-Induced Platelet Aggregation by Web 2086 'in-Vitro', an Antagonist to the Receptor for Platelet-Activating Factor, in Bovine
Publication date :
1996
Journal title :
Journal of Veterinary Medicine. A, Physiology, Pathology, Clinical Medicine
ISSN :
0931-184X
eISSN :
1439-0442
Publisher :
Blackwell Publishing, Berlin, Germany
Volume :
43
Issue :
7
Pages :
399-413
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
CNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
Funding text :
Bastos is a recipient of a grant from CNPq and FCAP Belém-Parà Brazil
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Bibliography
BIRKE, F. W., and K. H. WEBER, 1988: Specific and high affinity binding of WEB 2086 to human platelet PAF receptors. Clin. Exper. Pharmacol. Physiol. Suppl. 13, 2.
BONDY, G. S., and P. A. GENTRY, 1989: Characterization of the normal bovine platelet aggregation response. Comp. Biochem. Physiol. C92, 67-72.
BORN, G. V. R., and M J. CROSS, 1963: The aggregation of blood platelets J. Physiol. (Lond), 168, 178-195.
BRAQUET, P., L. TOUQUI, T. Y. SHEN, and B. B. VARGAFTIG, 1987: Perspectives in platelet-activating factor research Pharmacol. Rev. 39, 97-145.
CARGILL, D. I, D. S. COHEN, R. G. VAN VALEN, J. J. KLINFK and R. P. LEVIN, 1989: Aggregation, release and desensitization induced in platelets from five species by platelet activating factor (PAF). Thromb. Haemost. 49, 204-207.
CASALS-STENZEL, J., and K. H. WEBER, 1987: Triazolodiazepines: dissociation of their PAF (platelet-activating factor) antagonistc and CNS activity. Br. J. Pharmac. 90, 139-146.
CHAN, W. P., and J V. LEVY, 1991: Effects of antiplatelet agents on platelet aggregation induced by platelet-activating factor (PAF) in human whole blood Prostaglandins 42, 337-342.
CHAP, H., G. MAUCO, M. F. SIMON, J. BENVENISTE, and L. DOUSTE-BLAZY, L., 1981: Biosynthetic labelling of platelet activating factor from radioactive acetate by stimulated platelets. Nature (Lond.) 289, 312-314
CHIGNARD, M., J. P. LE COUEDIC, M. TENCE, B. B. VARGAFTIG, and J. BENVENISTE, 1979: The role of platelet-activating factor in platelet aggregation. Nature 279, 799-800
CHUNG, K. F., 1992: Platelet-activating factor in inflammation and pulmonary disorders. Clin. Sci. 83, 127-138.
CUSAK, N. J., 1980: Platelet-activating factor. Nature 285, 22.
DAVID, J.-L., F. MONFORT, F. HERION, and R. RASKINET, 1979: Compared effects of three dose-levels of Ticlopidine on Platelet function in normal subjects. Thromb. Res. 14, 35-49.
FOSTER, A. P., P. LEES, M. J. ANDREWS, and F. M. CUNNINGHAM, 1992: Effects of WEB 2086, an antagonist to the receptor for platelet-activating factor (PAF), on PAF-induced responses in the horse. Equine Vet. J. 24, 203-207.
FOSTER, A. P., F. M. CUNNINGHAM, M. J. ANDREWS, and P. LEES, 1993: A comparison of the action of platelet factor (PAF) antagonists WEB2170 and 2086 in the horse. J. Vet. Pharmacol. Ther. 16, 477-487.
GODFROID, J. J., F. HEYMANS, E. MICHEL, C. REDEVILH, E. STEINER, and J. BENVENISTE, 1980: Platelet-activating factor (PAF-acether): Total synthesis of 1-0-octadecyl 2-0-acetyl sn-glycero-3-phosphorylcoline. FEBS Lett. 116, 161-164.
GROUSE, L. H., G. H. R. RAO, D. J. WEISS, V. PERMAN, and J. G. WHITE, 1990: Surface-activated bovine platelets do not spread, they unfold. Am. J. Pathol. 136, 399-408.
KENAKIN, T. P., 1987: Pharmacological analysis of drug receptor interaction. pp. 210-217, Raven, New York.
KOJIMA, S., H. HAGIWARA, W. SOGA, F. SEKIYA, Y. SAITO, and Y. INADA, 1987: Cooperativity between platelet-activating factor and collagen in platelet aggregation. Biochem. Biophys. Res. Commun. 145, 915-920.
KOJIMA, S., F. SEKIYA, Y. INADA, T. TSUKADA, and Y SAITO, 1990: Cooperativity between platelet-activating factor and collagen in aggregation of bovine platelets III. FEBS Lett. 267, 226-228.
KORNECKI, E., 1984: Platelet-activating factor-induced aggregation of human platelets specifically inhibited by Triazolodiazepines. Science 226, 1454-1456.
KORTH, R., M. HIRAFUJI, C. L. KERALY, D. DELAUTIER, J. BIDAUT, and J. BENVENISTE, 1989: Interaction of the Paf antagonist WEB 2086 and its hetrazepine analogues with human platelets and endothelial cells. Br. J. Pharmacol. 98, 653-661.
LEVY, J. V., and K. EZZET, 1987: Schild plot analysis of six putative antagonist of platelet activating factor (PAF) on human platelets. Pharmacologist 29, 219.
LIGGITT, H. D., R. W. LEID, and L. HUSTON, 1984: Aggregation of bovine platelets by acetyl gryceril ether phosphorylcholine (Platelet activating factor). Veterinary Immunol. Immunopathol. 7, 81-87.
MARCUS, A. J., L. B. SAFIER, and H. L. ULLMAN, 1981: Effects of acteyl glyceryl ether phosphorylcholine on human platelet function in vitro. Blood 58, 1027-1031.
MATTHIAS, T. T., 1987: Blood coagulations disorders, Chap. 1. Springer Verlag. Berlin-Heidelberg. p. 19-29.
MEADE, C. J., H. HEUER, and R. KEMPE, 1991: Biochemical pharmacology of platelet-activating factor (and PAF antagonists) in relation to clinical and experimental thrombocytopenia. Biochem. Pharmacol. 41, 657-668.
MEYERS, K. M., J. B. KATZ, R. M. GLEMMONS, J. B. SMITH, and H. HOLMSEN, 1980: An evaluation of the arachidonate pathway of platelets from companion and food-producing animals, mink and man. Thromb. Res. 20, 13-24.
MCCULLOCH, R. K., AND R. VANDOGEN, 1990: Mechanism of platelet activating factor-induced aggregation and secretion in human platelets. Prostaglandins 39, 13-21.
MCMANUS, L. M., D. J. HANAHAN, and R. N. PINCKARD, 1981: Human platelet stimulation by acetyl glyceryl ether phosphorylcholine. J. Clin. Invest. 67, 903-906.
NAMM, D. H., A. S. TADEPALLI, and J. A. HIGH, 1982: Species specificity of the platelet responses to 1-0-alkyl-2-acetyl-sn-glycero-3phosphocholine. Thromb. Res. 25, 341-350.
O'DONNEL, S. R., and C. J. K. BARNETT, 1988: PA2 values for antagonists of platelet activating factor on aggregation of rabbit platelets. Br. J. Pharmacol. 94, 437-442.
RAUCHLE, K L., S. R. O'DONNELL, C. J. K. BARNNETT, and X-P. ZENG, 1989: A comparison of the heterazepine PAF antagonists WEB2086, WEB2170 and STY2180. Clin. Exp. Pharmacol. Physiol. suppl 14, Abstract 176.
SAUDERS, R. N., and D. A. HANDLEY, 1987: Platelet-activating factor antagonists. Ann. Rev. Pharmacol. Toxicol. 27, 237-255.
SCHORDERET, M., 1988: Pharmacologie. Des concepts fondamentaux aux applications thérapeutiques. Frison-Roché, Paris. Slaktine, Ed. Slaktine, p. 3-19.
SOLOVIEV, A. I., and P. BRAQUET, 1992: Platelet-activating factor - A potent endogenous mediator responsible for coronary vasospasm. NIPS 7, 166-172.
SPENCE, D. P. S., S. L. JOHNSTON, P. M. A. CALVERLEY, P. DHILLON, C. HIGGINS, E. RAMHAMADY, S. TURNER, A. WINNINHG, J. WINTER, and S. T. HOLGATE, 1994: The effect of the orally active Platelet-activating factor antagonist WEB 2086 in the treatment of Asthma. Am. J. Respir. Crit. Care Med. 149, 1142-1148.
STEEL, R. G. D., and J. M. TORRIE, 1980: Principles and procedures of statistics a biometrical approach. McGraw-Hill International Editions - Statistics Series, New York. 2nd. edn, p. 185-186.
STEWART, A. G., and G. J. DUSTING, 1988: Characterization of receptors for platelet-activating factor on platelets, polymorphonuclear leukocytes and macrophages. Br. J. Pharmacol. 94, 1225-1233.
SUQUET, C. M., and R. W. LEID, 1983: Aggregation of equine platelets by PAF (Platelet-activating factor), Inflammation 7, 197-203.
TAHRAOUI, L., A. FLOCH, S. MONDOT, and I. CAVERO, 1988: High affinity specific binding sites for tritiated platelet-activating factor in canine platelet membranes: Counterparts of platelet-activating factor receptors mediating platelet aggregation. Mol. Pharmacol. 34, 145-151.
UKENA, D., G. DENT, C. ROBAUT, F. W. BIRKE, G. W. SYBRECHT, and P. J. BARNES, 1988: Radioligand binding of antagonists of platelet-activating factor to intact human platelet. FEBS Lett. 228, 285-289.
VARGAFTIG, B. B., M. CHIGNARD, and J. BENVENISTE, 1981: Present concepts on the mechanism of platelet aggregation. Biochem. Pharmacol. 30, 263-271.
VIEIRA, S., 1985: Introdução a Bioestatística. 3a. ed. pp. 223-245, Editora Campus Ltda, Rio de Janeiro.
WHITE, J. G., 1987: The secretory pathway of bovine platelets. Blood 69, 878-885.
ZUCKER-FRANKIN, D., K. A. BENSON, and M. M. KENNETH, 1985: Absence of a surface-connected canalicular system in bovine platelets. Blood 65, 241-244.
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