2-[3-[2-(4,5-diphenyl-2-oxazolyl) ethyl] phenoxy] acetic acid (BMY 42393): 2). Oral activity and efficacy in animal models of arterial thrombosis.
Thromb Res
; 74(2): 125-33, 1994 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-8029813
ABSTRACT
The oral activity and antithrombotic efficacy of BMY 42393 was examined in ex vivo platelet aggregation studies and arterial thrombosis animal models. In a heterologous ex vivo platelet aggregation assay, ADP-induced human platelet aggregation was inhibited when washed human platelets were combined with rat platelet-poor plasma, taken from rats previously orally-dosed with BMY 42393. The IC50 for platelet aggregation inhibition was approximately 10 mg/kg. In a laser-induced thrombosis model, thrombus formation in a revascularized rabbit ear chamber was prevented in a dose-dependent fashion with an ED50 of about 2 mg/kg. A relatively long duration of anti-thrombotic activity was observed in the rabbit ear laser-induced thrombus study and the ex vivo platelet studies. Inhibition of thrombus formation was also demonstrated in a canine model of electrically-induced coronary artery thrombosis. BMY 42393 also prevented cyclic flow reductions in a monkey stenotic renal artery model. These studies indicate that BMY 42393 is orally active and capable of preventing laser and electric current-induced thrombus formation in animal models of arterial thrombosis.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oxazoles
/
Fenoxiacetatos
/
Trombosis Coronaria
Límite:
Animals
/
Humans
/
Male
Idioma:
En
Revista:
Thromb Res
Año:
1994
Tipo del documento:
Article