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作 者:徐斌[1] 李育[1,2] 章嫡妮[1] 林超[1] 钱星[1] 李伟[1] 卞慧敏[1,3]
机构地区:[1]南京中医药大学药学院 [2]基础医学院 [3]江苏省中药药效与安全性评价重点实验室,江苏南京210046
出 处:《中国药理学通报》2015年第3期367-374,共8页Chinese Pharmacological Bulletin
基 金:国家自然科学基金资助项目(No 81072542);教育部博士点基金资助项目(No 20123237110010);江苏省自然科学基金资助项目(No BK2011077);江苏省高校优势学科建设工程资助项目
摘 要:目的研究Liguzinediol对普萘洛尔所致豚鼠急性心衰模型的治疗作用并评价其效能、效价和治疗指数。方法静脉注射普萘洛尔建立豚鼠急性心力衰竭(AHF)模型后,分组静脉恒速注射给予Liguzinediol(2.85、5.70、11.40、22.80、45.60、91.20 mg·kg-1)及阳性药盐酸肾上腺素(0.31 mg·kg-1),用RM6240多道生理信号采集处理系统记录给药0、5、10、20、40、60、90和120 min时左心室内压最大上升/下降速率(±dp/dtmax)、左心室内压(LVSP)、动脉收缩压(MSP)、动脉舒张压(MDP)和心率(HR)的变化;计算该药的效能、效价和治疗指数。结果 Liguzinediol(11.40、22.80和45.60 mg·kg-1)能有效升高模型豚鼠+dp/dtmax、LVSP、MSP、MDP和HR,降低-dp/dtmax,Liguzinediol(2.85、5.70mg·kg-1)作用较弱,ED50约为12.93 mg·kg-1,治疗指数(LD50/ED50)为131,45.60 mg·kg-1已达最大效能,再加大剂量至91.20 mg·kg-1其效应并不能相应增强。结论 Liguzinediol对急性心衰豚鼠的血流动力学指标有明显的改善作用,其安全性比同类药物高。Aim To study the effect of liguzinediol on cardiac function in acute heart failure (AHF) guinea pig induced by propranolol, and evaluate its efficacy, potency and therapeutic index. Methods The AHF model in guinea pigs was copied by propranolol. Dif- ferent doses of liguzinediol ( 2. 85, 5.70, 11.40, 22. 80, 45.60 and 91.20 mg · kg-1 ) and adrenaline hydrochloride (0.31 mg~ kg-1 ) were injected intrave- nously. The changes of the + dp/dt LVSP, MSP, MDP and HR were recorded by RM6240 system after the administration in 0, 5, 10, 20, 40, 60, 90 and 120rain. The efficacy, potency and therapeutic index of liguzinediol were calculated finally. Results Com- pared with model group, these doses of liguzinediol (2. 85, 5.70 and 91.20 mg· kg-1 ) could significant-ly increase the + dp/dt MSP, MDP, HR, and de- crease-dp/dt and the effect of these doses of ligu- zinediol (2.85 and 5.70 mg · kg-1) were weak. Through the calculation, the EDs0 of liguzinediol was about 12.93 mg /kg-1 and its therapeutic index (LDso/EDso) was 131. The 45.60 mg · kg-1 dose of liguzinediol was its maximum efficiency, and its effect could not improve even the dose was increased to 91.20 mg · kg-1. Conclusion Liguzinediol can sig- nificantly improve the hemodynamic parameters in AHF guinea pigs, and it is of more safety than other similar drugs.
关 键 词:LIGUZINEDIOL 豚鼠急性心力衰竭模型 血流动力学 效价 效能 治疗指数
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