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为了研究重组人的GABAA受体复合物A_2β_2γ_2s （A_2亚基是α1亚基148氨基酸由异亮氨酸突变为缬氨酸）的药理学特征，阐明哪一个氨基酸是影响受体亲和性的关键，通过定向位点突变，我们构建了A_2亚基151天冬氨酸突变为天冬酰胺和A_2亚基149苏氨酸突变为谷氨酰胺，并通过baculovirus病毒-Sf-9昆虫表达系统重组了A_2亚基151天冬氨酸突变为天冬酰胺和A_2亚基149苏氨酸突变为谷氨酰胺与β_2，γ_2s 亚基的GABA_A 受体复合物，测定了6个GABA_A 受体GABA位点活性化合物。发现拮抗剂pitrazepine亲和力下降了约10倍，本研究结果表明，149和151位氨基酸很有可能是影响pitrazepine对含有α1亚基的GABA_A 受体复合物亲和性、药效的关键。
In order to investigate the pharmacological properties of recombinant human GABAA receptor complex A_2β_2γ_2s (A_2 subunit is the mutation of 148 amino acids from isoleucine to valine in the α1 subunit), it is clarified which amino acid is the key factor influencing receptor affinity , We constructed the mutation of A_2 subunit 151 aspartate to asparagine and the A_2 subunit 149 threonine to glutamine through directional site mutation and recombined by Baculovirus virus-Sf-9 insect expression system A_2 aspartate from asparagine to asparagine and A_2 subunit 149 threonine mutated to GABA_A receptor complex between glutamine and β_2, γ_2s subunits, GABA activity of 6 GABA_A receptors was measured Compound. Found that the antagonist pitrazepine affinity decreased about 10-fold, the results of this study showed that 149 and 151 amino acids is likely to affect the pitrazepine α1 subunit containing GABA_A receptor complex affinity, the key.