RESUMO
We investigated the effect of a new indole derivative Sbt-828 with antiaggregant properties on prostacyclin-generating activity of the vascular wall and thromboxane A2 level in platelets of intact rats. The substance under study did not affect prostacyclin production by the vascular wall and significantly reduced thromboxane A2 level, being superior to the reference drug acetylsalicylic acid by 1.6 times, as seen from reduced malonic dialdehyde level in the thrombin-induced rat platelets.
Assuntos
Plaquetas/efeitos dos fármacos , Epoprostenol/sangue , Indóis/farmacologia , Inibidores da Agregação Plaquetária/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Tromboxano A2/sangue , Animais , Animais não Endogâmicos , Aorta Abdominal/efeitos dos fármacos , Aorta Abdominal/metabolismo , Aspirina/farmacologia , Plaquetas/citologia , Plaquetas/metabolismo , Epinefrina/antagonistas & inibidores , Epinefrina/farmacologia , Indóis/síntese química , Injeções Intravenosas , Dose Letal Mediana , Masculino , Malondialdeído/sangue , Inibidores da Agregação Plaquetária/síntese química , Ratos , Trombina/antagonistas & inibidores , Trombina/farmacologia , Técnicas de Cultura de TecidosRESUMO
Antithrombotic properties of a new P2Y1 receptor antagonist N-[(1-morpholinopropyl-amino)- carbonyl-2-(1-ethyl-1H-indole-3-yl)-vinyl]-4-methylphenyl-amide hydrochloride, substance Sbt-119, and reference drug ticlopidine were studied on experimental models of arterial and systemic thromboses. Substance Sbt-119 was 39.9% (p<0.05) more potent than ticlopidine in producing the antithrombotic effect. Moreover, substance Sbt-119 was shown to increase the survival rate of animals after systemic treatment with ADP (by 20%, p<0.0001). This substance decreased the number of mural thrombi and reduced the severity of hemodynamics disturbances in the organs during systemic thrombosis.