孟鲁司特对离体支气管哮喘豚鼠呼吸道平滑肌的效应

The effect of Montelukast on the airway smooth muscle isolated from asthmatic guinea pigs

目的探讨孟鲁司特（MTL）对离体支气管哮喘（哮喘）豚鼠呼吸道平滑肌（ASM）的效应。方法取哮喘豚鼠支气管制作成气管螺旋条，分成MTL组、MTL＋硝苯地平组、MTL＋格列苯脲组、MTL＋普萘洛尔组、MTL＋阿托品组和对照组。观察ASM在静息张力下，各组不同MTL浓度对ASM的效应并比较各组间ASM舒张率。结果MTL在浓度10^-7.5～10^-3．0mol／L时对离体哮喘豚鼠ASM具有舒张作用[（0．31±0．12）％-（99．61±0．40）％]，与对照组[0～（12．77±0．33）％]比较差异均有统计学意义（P均〈0．05）。离体哮喘豚鼠ASM静息张力下，各组与MTL组比较，MTL＋硝苯地平组在MTL浓度10^-6.0～10^-3．5mol／L时，舒张作用明显加强[（11．48±1．63）％～（94．03±1．87）％]，与各组之间两两比较差异有统计学意义（P均〈0．05）；MTL＋普萘洛尔组在MTL浓度10^7.5～10^-6．5mol／L时，舒张作用明显减弱[（0．16±0．07）％-（2．73±0．84）％]，与各组之间两两比较差异有统计学意义（P均〈0．05）；MTL＋格列苯脲组、MTL＋阿托品组在MTL浓度10^-8.0～10-3．0mol／L时，舒张作用与各组之间两两比较差异无统计学意义（P均〉0．05）。结论MTL可对离体哮喘豚鼠ASM静息张力产生明显的舒张作用，其效应的产生与抑制Ca^2＋内流有关，可能是通过激动ASM上的β2受体导致ASM舒张。

Objective To observe the effect of Montelnkast （MTL） on the airway smooth muscle（ASM） isolated from asthmatic guinea pigs. Methods The bronchus of asthmatic guinea pigs were made into trachea spiral. These bronchus were divided into 6 groups ： MTL group, MTL ＋ Nifedipine group, MTL ＋ Glibenclamide, MTL ＋ Prop- ranolol group, MTL ＋ Atropine group and control group. The effect of different concentrations of MTL on the ASM in the resting tension was observed and the ASM relaxation pigs were compared among the groups. Results MTL in 10 ^-7.5 - 10 ^-3.0 mol/L had diastolic effect on the asthmatic guinea pigs ASM [ （0. 31 ± 0. 12） % - （ 99.61 ± 0.40） % ], and compared with the control group, there were significant differences [ 0 - （ 12.77 ± 0.33 ） %, all P 〈 0.05 ]. In the resting tension of asthmatic guinea pig ASM [ （ 11.48 ± 1.63 ） % - （94.03 ± 1.87） % ] , the diastolic function was remarkably improved at 10^-6.0 -10^ -3.5 mol/L of MTL in MTL ＋ Nifedipine group, and the differences among the groups had statistical significance （all P 〈 0.05 ）. The diastolic function was antagonism at 10^-7.5 - 10^-6.5 mol/L of MTL in MTL ＋ Propranolol group [ （0.16 ± 0.07 ）% - （2.73 ± 0.84 ）% ] and the differences among the groups had statistical significance （all P 〈 0.05）. The diastolic function had no significant difference between 10^-8.0 - 10 ^3.0 mol/L of MTL in MTL ＋ Atropine group and MTL ＋ Glibenclamide group （ all P 〉 0.05）. Conclusions It has diastolic function for MTL on the isolated asthmatic guinea pigs ASM in the resting tension. The effect may be related with inhibitor of Ca^2＋ internal flow and the competitive exciting β2 receptor.