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具有血管作用的保护精氨酸的合成

顾鸣镝, 彭师奇, 于学敏, 蔡孟深, 郭雪清, 张连元, 董淑云, 张越, 唐朝枢   

  1. 北京医科大学, 北京 100083
  • 收稿日期:1992-08-26 修回日期:1993-08-23 出版日期:1993-12-15 发布日期:1993-12-15

The Synthesis of Vasoactive Protected L-Arginine

Ming-Di Gu, Shi-Qi Peng, Xue-Min Yu, Meng-Shen Cai, Xue-Qing Guo, Lian-Yuan Zhang, Shu-Yun Dong, Yue Zhang, Chao-Shu Tang   

  1. Beijing Medical University; Beijing 100083
  • Received:1992-08-26 Revised:1993-08-23 Online:1993-12-15 Published:1993-12-15

摘要: 在二氧化酶作用下, L-精氨酸转变为 L-胍氨酸和 NO, NO 显示 EDRF 样的重要的生物活性。NG-nitro-L-arginine 在体外和体内都抑制 EDRF 的生物合成, EDRF 有效拮抗剂。本文研究结果表明 NG-nitro-L-arginine HCl·NGO2-NO2-L-Arg-OCH3在体外有血管舒张作用, 但是这两个化合物在体内对动脉血压具有剂量依赖的增加效应。在体外 HCl·NGO2-L-Arg-NG-NO2-L-Arg-OCH3 NE 收缩的鼠动脉肌条有舒张作用, 而在体内它具有两向性。例如低剂量时可使大鼠平均动脉血压(MAP)降低, 而高剂量时使 MAP 增高。NG-Tos-L-Arg-NG-Tos-L-Arg-OH 具有剂量依赖关系的舒血管作用和降低血压的活性。

关键词: 血管作用, 保护的 L-精氨酸, EDRF 样效应

Abstract:

Under the catalysis of dioxygenase L-arginine is converted to L-citrulline and nitric oxide, the latter exhibits endothelium derived relaxing factor(EDRF)-like actions.NG-nitro-L-arginine has an inhibitory effect on the biosynthesis of EDRF in vitro and in vivo, hence it is an EDRF antagonist.The results of the present work indicate that both NG-NO2-L-Arg-OH and HCl·NG-NO2-L-Arg-OCH3 have vasodilating effect in vitro, but produced dose-depending increase in mean arterial blood pressure (MAP) in vivo.In vitro HCl·NG-NO2-L-Arg-NG-NO2-L-Arg-OCH3 relaxed rat aortic strip pretreated with noradrenaline(NE).In vivo, however, it produced biphasic effect, i.e, decreased MAP at lower dose and increases MAP at higher dose, NG-Tos-L-Arg-NG-Tos-L-Arg-OH produced dose-depending vasodilating and hypotensive actions.

Key words: Vasoactive, Protected L-arginine, EDRF-like functions

Supporting: