BM-13505抗栓作用及机理研究

BM-13505抗栓作用及机理研究

王福军, 张世玲

山东医科大学药学系药理教研室, 济南 250012

收稿日期:1993-02-18 修回日期:1994-09-07 出版日期:1995-06-15 发布日期:1995-06-15

Antithrombotic Effects of BM-13505, a ThromboxaneReceptor Antagonist

Fu-Jun Wang, Shi-Ling Zhang

Dpepartment of Pharmacology; Faculty of Pharmacy; Shandong Medical University; Jinan 250012

Received:1993-02-18 Revised:1994-09-07 Online:1995-06-15 Published:1995-06-15

摘要/Abstract

摘要：

BM-13505是新合成的血栓烷受体拮抗剂, BM-13505 0.45和0.23 mg/kg iv延长大鼠颈动脉血管阻塞时间 (P<0.00 1 and <0.01)。BM-13505 2 mg/kg iv有效地防止AA 4 mg/kg所致的大鼠脑血栓形成(P<0.01)。BM-13505 10 mg/kg ip可防止AA诱导的小鼠肺部栓塞(P<0.01)。该药可延长小鼠尾出血时间。BM-13505显著抑制AA诱导的兔血小板聚集, 半数抑制浓度IC50为0.17 μmol/L, 对ADP和胶原诱导的血小板聚集无影响。BM-13505降低兔血小板及小鼠血浆中TXB2水平, 对血小板cAMP水平无影响。在不远的将来, BM-13505可能会发展成一种理想的抗血小板药及抗血栓药。

关键词: BM13505, 血栓形成, 出血时间, 血小板聚集

Abstract: BM-13505 is a new type of thromboxane receptor antagonist developed first abroad and synthesized in our school, with a modifed method recently. The results of our study showed that the occlusion time of carotid artery in experimental thrombosis rats was prolonged by BM-13505, 0.45 and 0.23 mg/kg iv (P<0.00 1 and <0.01 respectively). BM-13505 2 mg/kg iv effectively prevented the cerebral thrombosis caused by AA 4 mg/kg in rats (P<0.01) BM-13505 10 mg/kg ip prevented the AA-induced pulmonary thrombosis in mice (P<0.01). Tail bleeding time of mice was prolonged by this dru.BM-13505 significantly inhibited the AA-induced rabbit platelet aggregation, with an IC50 of 0.17 μmol/L; ADP-and collagen-induced aggregations were not affected.TXB2 level in platelets and that in mice plasma were decreased by BM-13505, but cAMP level in platelets was not affected. BM-13505 may be possibly developed into a useful anti-platelet and anti-thrombotic drug.

Key words: BM-13505, Thrombosis, Platelet aggregation, Thromboxane receptor antagonist

Supporting:

王福军, 张世玲. BM-13505抗栓作用及机理研究[J]. .

Fu-Jun Wang, Shi-Ling Zhang . Antithrombotic Effects of BM-13505, a ThromboxaneReceptor Antagonist[J]. .

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