摘要
BM-13 505 is a new type of thromboxane receptor antagonist developed firstabfoad and synthesized in our school.wita modife 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 mglkg iv fP<0.00 1 and <0.01 respectively).B·13505 2 mgjkg iv ef fectively 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 IC￣(50) of0.17 μmol/L; ADp-and collagen-induced aggregations were not affected.TXB_2 level in platelets and that in mice plasma were decreased by BM-13505,but cAMP level inplatelets was not affected. BM-13505 may be possibly developed into a useful anti-platelet and anti-thromboti c drug。
ＢＭ１３５０５是新合成的血栓烷受体拮抗剂，ＢＭ１３５０５０．４５和０．２３ｍｇ／ｋｇｉｖ延长大鼠颈动脉血管阻塞时间（ｐ＜０．００１和ｐ＜０．０１）．ＢＭ１３５０５２ｍｇ／ｋｇｉｖ有效地防止ＡＡ４ｍｇ／ｋｇ所致的大鼠脑血栓形成（ｐ＜０．０１）。ＢＭ１３５０５１０ｍｇ／ｋｇｉｐ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。ＢＭ１３５０５显著抑制ＡＡ诱导的兔血小板聚集，半数抑制浓度ＩＣ＿（５０）为０．１７Ｖｍｏｌ／Ｌ，对ＡＤＰ和胶原诱导的血小板聚集无影响。ＢＭ１３５０５降低兔血小板及小鼠血浆中ＴＸＢ＿２水平，对血小板ｃＡＭＰ水平无影响。在不远的将来，ＢＭ１３５０５可能会发展成一种理想的抗血小板药及抗血栓药。
