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Subunit-dependent interaction of the general anaesthetic etomidate with the γ-aminobutyric acid type A receptor

机译:全身麻醉药依托咪酯与γ-氨基丁酸A型受体的亚基依赖性相互作用

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摘要

It is concluded that the subtype of β-subunit influences the potency with which etomidate potentiates GABA-evoked currents and that the β isoform is a crucial determinant of the GABA-mimetic activity of this compound. The nature of the α-subunit also impacts upon the maximal potentiation and activation that the compound may elicit. Such pronounced influences may aid the identification of the site that recognizes etomidate. More generally, these results provide a clear example of structural specificity in anaesthetic action.
机译:结论是,β亚基的亚型影响依托咪酯增强GABA诱发的电流的效力,并且β同工型是该化合物的GABA模拟活性的关键决定因素。 α-亚基的性质也影响化合物可能引起的最大增强和活化。这种明显的影响可以帮助识别识别依托咪酯的部位。更一般地,这些结果提供了麻醉作用中结构特异性的明确实例。

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