Research Output
Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAAreceptor
  We have previously reported [(1991) EMBO J. 10, 3239–3245] the sequence of an invertebrate γ‐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 activate 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.

  • Type:

    Article

  • Date:

    03 August 1992

  • Publication Status:

    Published

  • Publisher

    Wiley-Blackwell

  • DOI:

    10.1016/0014-5793(92)80711-o

  • ISSN:

    0014-5793

  • Library of Congress:

    QH426 Genetics

  • Dewey Decimal Classification:

    576 Genetics & evolution

Citation

Zaman, S. H., Harvey, R. J., Barnard, E. A., & Darlison, M. G. (1992). Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAAreceptor. FEBS Letters, 307(3), 351-354. https://doi.org/10.1016/0014-5793%2892%2980711-o

Keywords

Benzodiazepine, Channel blocker, Cyclodiene insecticide: Invertebrate, Lymnaea stagnalis, GABA, receptor, Receptor activation; Xenopus oocyte expression

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