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目的:观察四氢孕酮与苯巴比妥的抗惊厥相互作用。方法:采用小鼠最大电休克惊厥(MES)试验,测定四氢孕酮和/或苯巴比妥的保护作用;并采用小鼠大脑皮质膜制备,用氚标氟硝安定检测四氢孕酮和/或苯巴比妥对GABA_A受体复合物的调节。结果:苯巴比妥(0.5-50mg·kg~(-1))对小鼠最大电休克惊厥具剂量依赖性的保护作用,其ED_(50)为2.61mg·kg~(-1),95％可信限为1.59-4.26mg·kg~(-1)。同样,四氢孕酮(0.01-1.0mg·kg~(-1))也有剂量依赖性的保护作用,其ED_(50)为0.11(0.06-0.18)mg·kg~(-1)。四氢孕酮和苯巴比妥联合用药(1:20)的ED_(50)为0.73(0.44-1.21)mg·kg~(-1),Q值小于1。测定四氢孕酮和/或苯巴比妥增加氚标氟硝安定的结合,其浓度效应曲线与功能性协同作用的理论曲线相符。结论:四氢孕酮和苯巴比妥对抗小鼠最大电休克惊厥有协同作用;两者对增加氚标氟硝安定与GABA_A受体复合物的结合也有功能性协同作用。
Objective: To observe the anticonvulsant interaction of tetrahydroprotetone and phenobarbital. Methods: The maximum electroconvulsive convulsive (MES) test in mice was used to determine the protective effect of tetrahydroprotropone and / or phenobarbital. The mouse cerebral cortex membrane was used to prepare tetrahydro progesterone And / or phenobarbital on GABA_A receptor complex regulation. Results: Phenobarbital (0.5-50 mg · kg -1) had a dose-dependent protective effect on the maximal electroshock convulsion in mice. The ED 50 value was 2.61 mg · kg -1, % Confidence limits of 1.59-4.26mg · kg -1. Similarly, tetrahydroprotetone (0.01-1.0 mg · kg -1) also had a dose-dependent protective effect with an ED 50 value of 0.11 (0.06-0.18) mg · kg -1. The ED 50 of the combination of progestin and phenobarbital was 0.73 (0.44-1.21) mg · kg -1 and the Q value was less than 1. Determination of the combination of tetrahydroprotetone and / or phenobarbital increases the triton-flunitrazepam concentration-response curve which corresponds to the theoretical synergy of the functional synergy. CONCLUSION: Tetrandrine and phenobarbital have synergistic effects on the maximal electroshock convulsions in mice. Both of them also have a synergistic effect on increasing the binding of triton-flunitrazepam and GABA_A receptor complex.