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目的 观察七氟醚作用下GABA与鼠脑突触膜上GABAA 受体结合的变化 ,揭示七氟醚可能的全麻分子作用机理。方法 采用放射配体结合分析法 (RBA) ,进行抑制试验及饱和试验 ,观察七氟醚作用下3 H GABA特异性结合量的变化。七氟醚浓度的测定用气相色谱法。结果 (1)七氟醚在反应液中的溶解有饱和趋势 ;(2 )抑制试验时复合物的放射性计数无明显变化 (P >0 0 5 ) ;(3)当反应液中七氟醚浓度为 15 5 6～ 5 8 75 μmol/L时 ,其KD值明显低于对照组 (P <0 0 5 ) ,实验组与对照组的Bmax无明显变化 (P >0 0 5 )。结论 七氟醚不直接作用GABA识别位点 ,七氟醚可提高GABA与GABAA 受体的亲和力 ,但不影响GABA的结合位点数
OBJECTIVE: To observe the changes of the binding of GABA to the GABAA receptor on the synaptic membrane of mouse brain under the action of sevoflurane and to reveal the molecular mechanism of action of sevoflurane in general anesthesia. Methods Radioligand binding assay (RBA) was used to determine the specific binding of 3 H GABA under the action of sevoflurane. Sevoflurane concentration was determined by gas chromatography. Results (1) The solubility of sevoflurane in the reaction solution tended to be saturated. (2) There was no significant change in the radioactivity count of the complex in the inhibition test (P> 0.05). (3) When the concentration of sevoflurane in the reaction solution KD was significantly lower than that of the control group (P <0 05) at 15 5 6 ~ 5 8 75 μmol / L. There was no significant difference in Bmax between the experimental group and the control group (P 0 05). Conclusion Sevoflurane does not directly affect the GABA recognition site. Sevoflurane can increase the affinity of GABA and GABAA receptor, but does not affect the binding sites of GABA