摘要
研究发现 ,哒嗪酮类化合物 96 12灌胃给药 (i.g)能有效抑制大鼠动 静脉旁路血栓形成 ,对胶原致肺血栓小鼠死亡也有较强的保护作用 .剂量为 75、15 0或 30 0mg/kg时 ,抑制率分别为36 0 4%、45 97%和 78 2 5 % ;保护率分别为 48%、6 4%和 72 % ;96 12 (i.g)剂量为 10 0mg/kg或 2 0 0mg/kg时 ,能使小鼠出血时间明显延长 ,延长率分别为 39 6 %和 76 3 % .放射免疫分析测定结果表明 96 12在终浓度为 1～ 10 0 μmol/L时能使洗涤兔血小板环磷酸腺苷水平明显升高 (P <0 0 0 1) .说明 96 12具有较强的抗血栓作用 ,升高血小板cAMP水平可能是其主要作用机理 .
In this paper,it was revealed that a novel pyridazinone 9612(i.g) was able to inhibit the thrombosis of rats by 36 04%,45 97% or 78 25% and protect mice from death induced by thrombotic chollenge in lungs 48,64% or 72% respectively while the dosage was 75,150 or 300 mg/kg.The bleeding time of the mice was prolonged by 39 6% or 76 3 % by 9612(ig)as the dosage was 100 or 200 mg/kg.The content of cAMP in the washed rabbit platelets was increased significantly( P <0 001) by 9612 as the final concentrations were 1～100 μmol/L.It is showed that 9612 has potent antithrombotic effect,its mechanism may be related with the increase of cAMP level in platelets.
出处
《沈阳药科大学学报》
CAS
CSCD
2000年第6期444-446,共3页
Journal of Shenyang Pharmaceutical University
关键词
哒嗪酮类化合物
血栓形成
环磷酸腺苷
pyridazinone
platelet
thrombosis
bleeding time
radioimmunoassay
adenosine cyclic monophospha
