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激动剂和惊厥拮抗剂对非洲爪蟾卵母细胞中表达的果蝇γ-氨基丁酸受体(Rdl)同型寡聚体的作用。

Actions of agonists and convulsant antagonists on a Drosophila melanogaster GABA receptor (Rdl) homo-oligomer expressed in Xenopus oocytes.

作者信息

Buckingham S D, Hosie A M, Roush R L, Sattelle D B

机构信息

Babraham Institute Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge, UK.

出版信息

Neurosci Lett. 1994 Nov 7;181(1-2):137-40. doi: 10.1016/0304-3940(94)90578-9.

Abstract

Cytoplasmic injection of Xenopus oocytes with cDNA-derived RNA (cRNA) encoding a wild-type Drosophila melanogaster GABA receptor subunit (Rdl) resulted in functional expression of a GABA receptor homo-oligomer. Membrane currents recorded in response to muscimol, trans (TACA)- and cis (CACA)-4-aminocrotonic acid reversed at membrane potentials close to ECl- and were insensitive to 1.0 x 10(-4) M bicuculline methiodide. An order of potency of GABA approximately muscimol approximately TACA > CACA > glycine was observed. Response of the expressed Drosophila Rdl receptor to GABA was reduced by t-butylbicyclophosphorothionate (TBPS), 4-n-propyl-4'-ethynylbicycloorthobenzoate (EBOB), picrotoxinin and the novel insecticide, fipronil (all at 1.0 x 10(-5) M).

摘要

将编码野生型黑腹果蝇γ-氨基丁酸(GABA)受体亚基(Rdl)的互补DNA(cDNA)衍生RNA(cRNA)胞质注射到非洲爪蟾卵母细胞中,导致了GABA受体同型寡聚体的功能性表达。记录到的对蝇蕈醇、反式(TACA)和顺式(CACA)-4-氨基巴豆酸的膜电流在接近氯离子平衡电位(ECl-)的膜电位处反转,并且对1.0×10⁻⁴ M甲基荷包牡丹碱不敏感。观察到GABA、蝇蕈醇、TACA、CACA、甘氨酸的效力顺序为:GABA≈蝇蕈醇≈TACA>CACA>甘氨酸。表达的果蝇Rdl受体对GABA的反应被硫代丁基双环磷酰三胺(TBPS)、4-正丙基-4'-乙炔基双环邻苯二甲酸酯(EBOB)、印防己毒素和新型杀虫剂氟虫腈(均为1.0×10⁻⁵ M)降低。

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