新型2,3-二甲基-2-丁胺衍生物对动脉平滑肌细胞钾通道功能的调节作用  

Effects of 2,3-dimethyl-2-butylamine derivatives on potassium channels in arterial smooth muscle cells from rats

作　　者：陈玉萍[1] 殷晓峰[2] 崔文玉[1] 杨日芳[1] 王林[1] 汪海[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]南京医科大学药理系,南京210029

出　　处：《中国药理学通报》2003年第5期525-529,共5页Chinese Pharmacological Bulletin

基　　金：国家 8 63计划重大专项课题;No 2 0 0 2AA2Z3 13 7

摘　　要：目的　研究 2 ,3 二甲基 2 丁胺化合物对动脉平滑肌钾通道的作用 ,分析其化学结构与钾通道调节作用之间的构效关系 ,从而初步推断其是否具有钾通道开放活性。方法　在急性分离的大鼠尾动脉平滑肌细胞上 ,采用膜片钳全细胞记录技术研究脂肪胺新结构衍生物对钾通道的影响。结果　通过对 14种化合物的研究发现 ,当一侧取代基碳原子数为 3～ 5个时 ,该类化合物对钾电流有明显的增强作用。结论　具有特定化学结构的 2 ,3 二甲基 2 丁胺衍生物对钾通道有激活作用 ,为一类新结构类型的钾通道开放剂。AIM To investigate the effects of newly synthesized 2,3-dimethyl-2-butylamine derivatives on potassium channels in single arterial smooth muscle cells from rats, to analyze the relationship between the compound structures and its regulation of potassium channels and then to evaluate their activities. METHOD Under whole-cell patch clamp conditions, the influences of those compounds on potassium currents were observed on the acutely isolated tail arterial smooth muscle cells. RESULTS Those compounds with three to five carbon branched alkyl could distinctly increase the outward potassium currents. CONCLUSION 2,3-dimethyl-2-butylamine derivatives area kind of newly potassium channel openers with especially chemical structures.

关 键 词：2 3—二甲基—2—丁胺衍生物 钾通道 动脉平滑肌细胞 膜片钳技术 

分 类 号：R329.24[医药卫生—人体解剖和组织胚胎学] R322.74[医药卫生—基础医学]