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研究美托洛尔对映体（＋）Ｍｅｔ和（－）Ｍｅｔ在麻醉自发性高血压大鼠的药物动力学药效学结合模型，比较两种对映体对其心血管系统的作用．方法：反相高效液相法测定血药浓度，生理记录仪观察药效，计算药动学及药动学药效学结合模型参数．结果：血药浓度时间曲线符合二室模型．Ｖｄ在两种Ｍｅｔ之间有显著性差异．药效和效应室浓度间的关系符合ｓｉｇｍｏｉｄＥｍａｘ模型．（＋）Ｍｅｔ抑制Ｖｍａｘ，ｄｐ／ｄｔｍａｘ和ＨＲ的Ｃｓｓ５０皆明显大于（－）Ｍｅｔ．结论：（＋）Ｍｅｔ和（－）Ｍｅｔ在ＳＨＲ存在着立体选择性分布，（－）Ｍｅｔ对其心血管系统的抑制作用强于（＋）Ｍｅｔ．
To study the pharmacodynamics-pharmacodynamic binding model of metoprolol enantiomers (+) Met and (-) Met in anesthetized spontaneously hypertensive rats and compare the effects of two enantiomers on the cardiovascular system effect. Methods: The plasma concentration was determined by reversed-phase high-performance liquid chromatography. The pharmacokinetics were observed by physiological recorder. The parameters of pharmacokinetic and pharmacokinetic-pharmacodynamic models were calculated. Results: The plasma concentration-time curve accorded with two-compartment model. Vd has a significant difference between the two Met. The relationship between potency and effect concentration is in accordance with the sigmoid-Emax model. (+) Met inhibited Vmax, dp / dtmax and HR of Css50 were significantly greater than (-) Met. Conclusion: The (+) Met and (-) Met show stereoselective distribution in SHR. (-) Met has stronger inhibitory effect on its cardiovascular system than (+) Met.