关键词: anticoagulant effect coagulation factor indobufen platelet factor.

Mesh : Animals Anticoagulants / chemistry pharmacokinetics pharmacology Blood Coagulation / drug effects Blood Coagulation Tests Dabigatran / pharmacokinetics Female Isoindoles / chemistry pharmacokinetics pharmacology Male Molecular Structure Partial Thromboplastin Time Phenylbutyrates / chemistry pharmacokinetics pharmacology Platelet Factor 3 / metabolism Platelet Factor 4 / metabolism Prothrombin Time Rabbits Rats Rivaroxaban / pharmacokinetics Thrombin Time

来  源:   DOI:10.3390/molecules23061452   PDF(Sci-hub)   PDF(Pubmed)

Abstract:
Indobufen is a new generation of anti-platelet aggregation drug, but studies were not sufficient on its anticoagulant effects. In the present study, the anticoagulant activity of indobufen was determined by monitoring the activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT) in rabbit plasma. We evaluated the anticoagulant mechanisms on the content of the platelet factor 3,4 (PF3,4), and the coagulation factor 1, 2, 5, 8, 10 (FI, II, V, VIII, X) in rabbits, as well as the in vivo bleeding time and clotting time in mice. The pharmacodynamic differences between indobufen and warfarin sodium, rivaroxaban, and dabigatran were further studied on thrombus formation and the content of FII and FX in rats. Animal experiments showed that intragastric-administrated indobufen can significantly reduce the APTT, PT, TT, PF3, FI, II, V, VIII, and X plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban. These results suggest that indobufen has some anticoagulant effects as strong as some conventional anticoagulants. The mechanism may be related to both exogenous and endogenous coagulation system.
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