γ-氨基丁酸（GABA）对苯二氮䓬激动剂和嘌呤取代苯二氮䓬拮抗剂结合的调节作用对比
Contrasting regulation by GABA of the displacement of benzodiazepine antagonist binding by benzodiazepine agonists and purines.
作者信息
Skerritt J H, Davies L P, Chow S C, Johnston G A
出版信息
Neurosci Lett. 1982 Oct 8;32(2):169-74. doi: 10.1016/0304-3940(82)90269-5.
Gaba increases the potency of the benzodiazepines chlordiazepoxide, clonazepam, diazepam, nitrazepam and oxazepam, and the triazolopyridazine CL 218,872 in displacing specific binding of the benzodiazepine antagonist [3H]Ro 15-1788. In contrast, the potencies of the purines 1-methyl- and 1-ethylisoguanosine for benzodiazepine antagonist binding sites were decreased by GABA, while the potencies of inosine, hypoxanthine, 6-dimethylaminopurine, and the non-benzodiazepine anxiolytic, zopiclone, were unaltered by GABA. The results suggest that the purines and 'classical' benzodiazepine agonists may bind to different conformations or populations of receptors.
γ-氨基丁酸（Gaba）可增强氯氮卓、氯硝西泮、地西泮、硝西泮和奥沙西泮等苯二氮卓类药物以及三唑并哒嗪CL 218,872在置换苯二氮卓拮抗剂[3H]Ro 15-1788特异性结合方面的效力。相比之下，嘌呤类药物1-甲基异鸟苷和1-乙基异鸟苷对苯二氮卓拮抗剂结合位点的效力会因γ-氨基丁酸而降低，而肌苷、次黄嘌呤、6-二甲基氨基嘌呤以及非苯二氮卓类抗焦虑药佐匹克隆的效力则不受γ-氨基丁酸影响。结果表明，嘌呤类药物与“经典”苯二氮卓类激动剂可能结合于不同构象或受体群体。
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