Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes

A. M. Hosie, Y. Shirai, S. D. Buckingham, J. J. Rauh, R. T. Roush, H. A. Baylis, D. B. Sattelle

    Research output: Contribution to journalArticlepeer-review

    Abstract

    The receptor antagonist actions are described for a novel bicyclic dinitrile compound (BIDN, 3,3-bis-(trifluoromethyl)-bicyclo [2.2.1] heptane-2,2-dicarbonitrile) on a Drosophila melanogaster homo-oligomeric GABA receptor expressed in Xenopus oocytes. BIDN blocked the wild-type form of the receptor in a neither purely competitive, nor purely non-competitive manner, being dependent on the GABA concentration yet insurmountable, and block was independent of the membrane potential. BIDN was found to be less effective against a mutant (A302 → S) form of the receptor resistant to dieldrin and picrotoxinin. This cross resistance of dieldrin-resistant receptors to BIDN is of interest in the light of recent findings that BIDN binding to insect membranes is displaced competitively by dieldrin, but not by picrotoxinin. © 1995 Elsevier Science B.V. All rights reserved.
    Original languageEnglish
    Pages (from-to)257-260
    Number of pages3
    JournalBrain research
    Volume693
    Issue number1-2
    DOIs
    Publication statusPublished - 25 Sept 1995

    Keywords

    • Bicyclic dinitrile
    • Convulsant site
    • Drosophila melanogaster
    • GABA receptor
    • RDL (resistance to dieldrin) subunit

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