氟哌啶醇季铵盐衍生物F_2对大鼠胸主动脉螺旋肌条收缩的影响  

Effect of Quaternary Ammonium Salt Derivative (F_2) of Haloperidol on Constrict ion of Isolated Rat Aorta Spiral Strips

作　　者：樊化平[1] 石刚刚[1] 郑锦鸿[1] 

机构地区：[1]汕头大学医学院药理学教研室,广东汕头515041

出　　处：《汕头大学医学院学报》2003年第2期67-69,共3页Journal of Shantou University Medical College

基　　金：国家自然科学基金 ( 3 0 0 70 3 0 4);广东省科技计划项目 (C3 0 10 4);广东省自然科学基金重点项目 ( 0 2 12 3 5 )

摘　　要：目的 :观察氟哌啶醇季铵盐衍生物F2 对KCl所致大鼠胸主动脉螺旋肌条收缩的影响 ,并初步探讨其作用机制。方法 :采用生物检定法 ,以大鼠胸主动脉螺旋条为标本 ,观察F2 (2× 10 - 6 、 6 32× 10 - 6 、 2× 10 - 5mol L)对KCl(10～4 0mmol L)诱导的肌条收缩的拮抗作用 ;F2 (10 - 4mol L)对 30、 80mmol LKCl所致收缩的拮抗作用 ,和格列苯脲 (10 - 6 ～ 10 - 4mol L)对F2作用的影响。结果 :F2 对KCl所致肌条收缩呈非竞争性拮抗 ,其拮抗作用呈量效关系 ,pD2 =5 13± 0 33。F2 (10 - 4mol L)可拮抗 80mmol L的KCl所致的肌条收缩。 10 - 6 ～10 - 4mol L的格列苯脲不能阻断 10 - 4mol L的F2 对 30mmol LKCl所致收缩的舒张效应。结论 :F2 呈非竞争性拮抗KCl所致大鼠主动脉螺旋肌条收缩。结合相关实验结果 ,F2 的拮抗作用可能与阻断血管平滑肌钙通道和开启钾通道有关 ,但这种钾通道不是ATP敏感性钾通道。Objective:To study the effect and mechanism of quate rnary ammonium sa lt derivative(F 2)of haloperidol on isolated rat thoracic aorta sp iral strips. Methods: Using the bioassay of rat aorta spiral strips, F 2( 2×10 -6 ?6 32×10 -6 ?2×10 -5 mol/L)was added into the bath medium prior to KCl(10～40mmol/L)admi nistration to observe the effect of F 2 on dose respons e curve of constriction in duced by KCl, respectively. The blocking effect of F 2(10 -4 mol/L)on the constriction induce d by KCl(30 and 80mmol/L)was recorded. The effects of F 2(10 -4 mol/L) and Glibe nclamide (10 -6 ～10 -4 mol/L)on the aorta strips were also observed. Results: F 2 d ecreased the constriction curve obviously in dose dependent manner(pD2=5 13 ±0 33). The constriction induced by KCl(80 mmol/L) was inhibited by F 2(10 - 4 mol/L). Glibenclamide did not counteract the diastolic effect of F 2 on the constricti on induced by KCl of 30 mmol/L. Conclusion: The constriction induced by KCl on rat aorta strips is inhibited by F 2. Refer to other related experiments, the effe ct of F 2 is due to blocking calcium channel and opening potassium channel which is not ATP sensitive type.

关 键 词：氟哌啶醇季铵盐衍生物F2 胸主动脉螺旋肌条收缩的影响 胸主动脉 钾通道 高血压 

分 类 号：R971.4[医药卫生—药品]