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兔iv咪苯嗪酮(CI—914)20 mg/kg,用RIA法测定其血浆中TXB_2和6—kcto—PGF_(1α)含量,给药后30 min和60 min.6—keto—PGF_(1α)/TXB_2比值显著升高(p<0.05).在用放射性TLC法进行的洗涤大鼠血小板~(14)C—AA代谢实验中,CI—914在2～500 μmol/L范围内以剂量依赖方式抑制大鼠血小板TXB_2生成,IC_(50)为51.5μmol/L,对HHT生成的抑制明显弱于对TXB_2生成的抑制作用;在相同剂量范围内,CI—914同时以剂量依赖方式使PGE_2,PGF_(2α)和PGD_2生成增加.在相同实验条件下,50μmol/L的已知的TXA_2合成酶抑制剂DAZ,与大剂量CI—914的实验结果类似.上述结果提示,CI—914对血小板TXA_2合成酶可能具有选择性抑制作用.
Rabbit iv imidazofenone (CI-914) 20 mg / kg, the contents of TXB2 and 6-kcto-PGF1α in plasma were measured by RIA method, the levels of TXB2 and 6-keto-PGF1 1α / TXB_2 was significantly increased (p <0.05) .In the platelet-to-14 C-AA metabolism assay of washed rats by radioactive TLC method, CI-914 was administered in a dosage of 2-500 μmol / Dependent manner inhibited the production of TXB_2 in rat platelets, IC 50 (51.5 μmol / L) inhibited the formation of HHT significantly less than that of TXB 2. In the same dosage range, CI-914 also induced PGE 2 , PGF_ (2α) and PGD_2 production increased.Under the same experimental conditions, 50μmol / L of known TXA_2 synthase inhibitor DAZ, similar to the experimental results of high dose of CI-914.The above results suggest that CI-914 on platelet TXA_2 synthase may have selective inhibitory effects.