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为了观察对苯丙氨基苯乙酸(BPAA)对喹诺酮类药物与人γ-氨基丁酸A(GABAA)受体的相互作用,本研究首次用重组人类GABA受体,通过放射配体结合竞争抑制实验方法,依次进行了联苯丁酮酸、BPAA对萘啶酸类喹诺酮抗菌药依诺沙星(enoxaxine)竞争抑制3H一蝇蕈醇与Sf-9膜表达GABAA受体亚型A2β2γ2s、A2β3γ2s、α2β3γ2s、α3β3γ2s和α5β3γ2s结合的实验。结果发现BPAA能明显增加依诺沙星对3H-蝇曹醇与各受体亚型的竞争抑制作用,IC50减小104-105倍,与BPAA相比,联苯丁酮酸的抑制作用较小,IC50减小102倍。本研究直接反映了联苯丁酮酸和BPAA与喹诺酮类药物在体内与GABAA受体的相互作用,其作用机制可能是两种药物发生了化学/分子作用,形成一种与GABAA受体有着极高亲和力的新结构。目前,本研究还在继续进行,验证喹诺酮类药物和BPAA之间的这种化学/分子作用。
In order to observe the interaction of quinacridone with human γ-aminobutyric acid A (GABAA) receptor by phenylalanine phenylacetic acid (BPAA), this study, for the first time, uses a recombinant human GABA receptor by radioligand binding competition inhibition assay Methods: Biphenylbutanoic acid and BPAA were used to compete with enoxaxine, a nalidixic acid quinolone antibacterial drug, for the inhibition of 3H-muscimol and Sf-9 membrane expression of GABAA receptor subtypes A2β2γ2s, A2β3γ2s, α2β3γ2s , Α3β3γ2s and α5β3γ2s binding experiments. The results showed that BPAA could significantly increase the inhibitory effect of Enoxacin on 3H-flies carotenol and the receptor subtypes, the IC50 was reduced by 104-105 fold. Compared with BPAA, the inhibitory effect of Buprofezate was small , IC50 is reduced by 102 times. This study directly reflects the interaction of bifendate and BPAA with quinolones in vivo and GABAA receptors, and its mechanism of action may be the chemical / molecular interaction of the two drugs to form a receptor with GABAA polar New structure with high affinity. Currently, this study is still ongoing to verify this chemical / molecular interaction between quinolones and BPAA.