摘要
用Ｌ－精氨酸及精氨酸－甘氦酸－天冬氨酸即ＲＧＤ序列的短肽精氨酸－甘氨酸－天冬氨酸－苯乙酰胺对正常血压及原发性高血压大鼠离体动脉血管的舒张作用进行了研究。结果发现：Ｌ－精氨酸和精氨酸－甘氨酸－天冬氨酸－苯乙酰胺对于两种动物的血管平滑肌均有程度不等的舒张作用，且该舒张作用显示出剂量依赖性和内皮依赖性。药效动力学分析表明，Ｌ－精氨酸和精氨酸－甘氨酸－天冬氨酸－苯乙酰胺舒张血管的半数有效浓度分别为１０－７和１０－６ｍｏｌ／Ｌ，二者Ａｃ－ＲＧＤ－ＰＥＡ最大舒张效应对于不同处置的不同动物约为４～２０％左右。实验结果提示Ｌ－精氨酸及其衍生物对于血压的调节及高血压的治疗有一定的作用。
The study investigated the effects of L-arginine and its analoguc Ac-Arc-Gly Asp-NHC2 H4C6H5(AC^RGD-PEA) in vascular tissucs of normotensive and hypertensiverats. Rat aortic rings, with or without endothelium, were suspended inorgan chambers for the measurement of isometric tension. L-arginine and Ac-RED-PEA evoked concentration-dependent relaxation in aortic rings both with and without endothelium arranged with 10-9 to 10+8 mol/L. Thevasodilater effects showed the endothelium dependence. The pharmacodynamic parameters exertedthat the half effective concentration (EGD) were 10-7 for L-arginine and 10-5 mol/L for Ac RGD-PAE respectively, both L-arginine and Ac-RGD-PAE maximum effects were responcesabout 4-20% vasodilation. The results suggesled that L-arginine and Ac-RGD-PEA may be arole in the regulation of bloodpressure and therapeutic effect for hypertension.
基金
国家自然科学基金
