Cloning and functional expression of a Drosophila y-aminobutyric acid receptor

Cloning and functional expression of a Drosophila y-aminobutyric acid receptor
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果蝇γ-氨基丁酸受体的克隆和功能表达

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通讯作者:
N. Lan
N. Lan
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作者:
Run;Delia;BELELLIt;J. Lambertt;John A. PETERSt;A. Reyes;N. Lan

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已从成虫 Droiwphla bead cDNA 库中分离出 cDNA e im a fI na amnobu-tric (GABA) 激活的 C1 通道。当在非洲爪蟾卵母细胞中表达时,该亚基功能主要以h Merk复合物的形式发挥作用,并被GABA或muuclmol激活。 GABA 诱发电流对 pcrox 的拮抗作用高度敏感,但对 b ue、RU 5135 或锌的拮抗作用尚不敏感。戊巴比妥极大地增强了 GABA 诱发的电流,我们较旧的 Sa-3a-d-20.oe 在 d 作用于 vereA GABA A 型受体时表现出巨大的效力和效果。尽管 zc 不敏感,但该亚基对结合也不敏感。因此,当与脊椎动物 GABA A 型受体或由 p 亚基组成的受体结合时,由该亚基形成的 GABA 受体表现出独特的 I aa。由于作为同聚体的受体,该亚基可能在旨在确定药物结合位点的许多研究中具有重要意义。这
A CDNA e im a fI na amnobu-tric (GABA)-activated C1 cannel has been olated fom an adult Droiwphla bead cDNA lbrry. When expresed In Xenopus laevis oocytes, the subunit funcion mefflclendy, pResmably as a h merk complex andis activated by GABA or muuclmol. GABA-evoked currents are hig sensitive to antag-onism by pcrox but are yetive to b ue, RU 5135, or zinc. Pentobarbitone greatly enhan GABA-evoked currents, w e the mnoerold Sa-3a-d-20.oe dem-onstrates a large red In both the potency and m effect when a d with Its actions upon vereA GABA ype A receptors. Aloug zc-insensive, the subunit is also insensiive to unite . Hence, the GABA receptors forned by this subunit exhibit a unique I aa when ared with vertebrate GABA type A reors or these composed of p subunis. Bam the recet e c ex tions as a homoo mer, tis subunit may be of valie in m ns studies aiming to define drug-binding sites. The