The effect of intravenous administration of WEB 2086 on PAF-induced platelet aggregation in healthy Friesian calves

被引:5
作者
DaSilva, MB
Gustin, P
Herion, F
Raskinet, R
David, JL
Gougnard, T
Plomteux, G
Desmecht, D
Lekeux, P
机构
[1] UNIV LIEGE,FAC VET MED,LAB PHARMACOL & TOXICOL,B-4000 LIEGE,BELGIUM
[2] UNIV LIEGE,CHU,THROMBOSIS HEMOSTASIS UNIT,B-4000 LIEGE,BELGIUM
[3] UNIV LIEGE,CHU,LAB CLIN TOXICOL,B-4000 LIEGE,BELGIUM
关键词
aggregation; cattle; chromatography; platelet; platelet-activating factor; platelet-rich plasma; thienotriazolodiazepine;
D O I
10.1023/A:1005950622207
中图分类号
S85 [动物医学(兽医学)];
学科分类号
0906 ;
摘要
The in vivo ability of the specific PAF-antagonist WEB 2086, a thienotriazolodiazepine, to inhibit platelet-activating factor (PAF) in cattle was investigated by in vitro determination of platelet aggregation curves. WEB 2086 was infused intravenously into a group of 5 healthy male Friesian calves in a dose of 3 mg/kg over 1 min. The resultant inhibition peaked between 30 min and 1 h after administration of WEB 2086. The inhibition was significantly reduced after 3 h and became non-0significant after 6 h, but maximal pre-treatment aggregation had not been restored by 24 h after the injection of WEB 2086. These results confirm previous results obtained in vitro and suggest that WEB 2086 is a potent antagonist of PAF activity in calves. They also suggest that further clinical studies with WEB 2086 in cattle are desirable.
引用
收藏
页码:521 / 531
页数:11
相关论文
共 34 条
[11]  
BRECHT HM, 1991, DRUG RES, V41, P51
[12]  
CASALSSTENZEL J, 1987, J PHARMACOL EXP THER, V241, P974
[13]   Inhibition of PAF-induced platelet aggregation by WEB 2086 'in-vitro', an antagonist to the receptor for platelet-activating factor, in bovine. [J].
daSilva, MB ;
Herion, F ;
Raskinet, R ;
David, JL ;
Gustin, P ;
Dessy, C ;
Lekeux, P .
JOURNAL OF VETERINARY MEDICINE SERIES A-ZENTRALBLATT FUR VETERINARMEDIZIN REIHE A-PHYSIOLOGY PATHOLOGY CLINICAL MEDICINE, 1996, 43 (07) :399-413
[14]   COMPARED EFFECTS OF 3 DOSE-LEVELS OF TICLOPIDINE ON PLATELET-FUNCTION IN NORMAL SUBJECTS [J].
DAVID, JL ;
MONFORT, F ;
HERION, F ;
RASKINET, R .
THROMBOSIS RESEARCH, 1979, 14 (01) :35-49
[15]  
DEMOPOULOS CA, 1979, J BIOL CHEM, V254, P9355
[16]   EFFECTS OF WEB-2086, AN ANTAGONIST TO THE RECEPTOR FOR PLATELET-ACTIVATING-FACTOR (PAF), ON PAF-INDUCED RESPONSES IN THE HORSE [J].
FOSTER, AP ;
LEES, P ;
ANDREWS, MJ ;
CUNNINGHAM, FM .
EQUINE VETERINARY JOURNAL, 1992, 24 (03) :203-207
[17]   PLATELET ACTIVATING FACTOR (PAF-ACETHER) - TOTAL SYNTHESIS OF 1-0-OCTADECYL 2-0-ACETYL SN-GLYCERO-3-PHOSPHORYL CHOLINE [J].
GODFROID, JJ ;
HEYMANS, F ;
MICHEL, E ;
REDEUILH, C ;
STEINER, E ;
BENVENISTE, J .
FEBS LETTERS, 1980, 116 (02) :161-164
[18]  
HENSON PM, 1976, FED PROC, V35, P516
[19]   INHIBITION OF THE BINDING AND AGGREGATION TO PAF INVITRO IN COMPARISON WITH PAF-ANTAGONISM INVIVO - AN INVESTIGATION USING DIFFERENT TYPES OF PAF-ANTAGONISTS [J].
HEUER, H ;
BIRKE, FW ;
CASALSSTENZEL, J ;
WEBER, KH .
PROSTAGLANDINS, 1988, 35 (05) :838-838
[20]  
HEUER H, 1989, DRUGS DESIGN DELIVER, V5, P33