Zaman S H, Harvey R J, Barnard E A, Darlison M G
MRC Molecular Neurobiological Unit, MRC Centre, Cambridge, UK.
FEBS Lett. 1992 Aug 3;307(3):351-4. doi: 10.1016/0014-5793(92)80711-o.
We have previously reported [(1991) EMBO J. 10, 3239-3245] the sequence of an invertebrate gamma-aminobutyric acid (GABA) type A (GABAA) receptor polypeptide which forms homo-oligomeric GABA-gated, bicuculline-sensitive, chloride-ion channels upon heterologous expression. We now demonstrate that the benzodiazepines Ro5-4864 (4'-chlorodiazepam) and diazepam, that are active at mammalian peripheral benzodiazepine sites, and not those benzodiazepines specific for central sites, directly active the homo-oligomeric receptor and evoke larger maximal responses than those elicited by GABA. In addition, members of the cyclodiene class of insecticides block the channel of the receptor in a manner indistinguishable from that of picrotoxin.
我们之前曾报道过[(1991)《欧洲分子生物学组织杂志》10, 3239 - 3245]一种无脊椎动物γ-氨基丁酸（GABA）A型（GABAA）受体多肽的序列，该多肽在异源表达时形成同聚寡聚体GABA门控、荷包牡丹碱敏感的氯离子通道。我们现在证明，在哺乳动物外周苯二氮䓬位点有活性的苯二氮䓬类药物Ro5 - 4864（4'-氯地西泮）和地西泮，而非那些对中枢位点特异的苯二氮䓬类药物，能直接激活同聚寡聚体受体，并引发比GABA所引发的更大的最大反应。此外，环二烯类杀虫剂以与印防己毒素难以区分的方式阻断受体通道。
