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具有抗血栓形成和血管舒张活性的新型一氧化氮供体,VIII:苯并噻唑-2(3H)-亚硝基胺

New NO-donors with antithrombotic and vasodilating activities, VIII: Benzothiazole-2(3H)-nitrosimines.

作者信息

Rehse K, Ciborski T, Lüdtke E

机构信息

Institut für Pharmazie, Freien Universität Berlin, Dahlem.

出版信息

Arch Pharm (Weinheim). 1994 Dec;327(12):771-7. doi: 10.1002/ardp.19943271204.

Abstract

Thirty title compounds were prepared and tested for their antiplatelet activity in the Born-test. Five nitrosimines inhibit the aggregation induced by collagen in concentrations below 10 mumol/L halfmaximally. Four compounds were investigated in an in vivo thrombosis model. An inhibition of thrombosis between 29 and 53% was observed in mesenteric arterioles of rats 2 h after p.o. administration (60 mg/kg). The effect in venoles was less pronounced (10-22%). For one compound these effects could still be demonstrated 4 h after oral application.

摘要

制备了30种目标化合物,并在博恩试验中测试了它们的抗血小板活性。5种亚硝基胺在浓度低于10 μmol/L时能半数最大程度地抑制胶原蛋白诱导的聚集。在体内血栓形成模型中研究了4种化合物。口服给药(60 mg/kg)2小时后,在大鼠肠系膜小动脉中观察到血栓形成受到29%至53%的抑制。在小静脉中的作用不太明显(10%至22%)。对于一种化合物,口服给药4小时后仍能证明这些作用。

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