Antiplatelet and Antithrombotic Properties of Compound L-36, a 6H-1,3,4-Thiadiazine Derivative.

V. Sirotenko, A. A. Spasov, A. Kucheryavenko, K. A. Gaidukova, A. V. Smirnov, Y. Velikorodnaya
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Abstract

Compound L-36, a new derivative of 6H-1,3,4-thiadiazine, was studied in in vitro and in vivo experiments. This compound exhibits high antiplatelet and antithrombogenic activity. In in vitro experiments, compound L-36 by its antiplatelet activity (by IC50) was superior to acetylsalicylic acid by 9.4 times. In in vivo experiments, compound L-36 by its ED50 value was close to the comparison drug. On the model of pulmonary artery thrombosis, compound L-36 ensured better survival of experimental animals than acetylsalicylic acid. Morphological studies showed that compound L-36 effectively attenuated the thrombosis processes in the pulmonary tissue induced by intravenous injection of a thrombogenic mixture (epinephrine and collagen).
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6H-1,3,4-噻二嗪衍生物 L-36 化合物的抗血小板和抗血栓特性
在体外和体内实验中研究了 6H-1,3,4-噻二嗪的新衍生物 L-36 化合物。该化合物具有很高的抗血小板和抗血栓形成活性。在体外实验中,化合物 L-36 的抗血小板活性(IC50)是乙酰水杨酸的 9.4 倍。在体内实验中,化合物 L-36 的 ED50 值与对比药物接近。在肺动脉血栓模型中,化合物 L-36 比乙酰水杨酸更能确保实验动物存活。形态学研究表明,静脉注射血栓形成混合物(肾上腺素和胶原蛋白)后,化合物 L-36 能有效减轻肺组织的血栓形成过程。
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