Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist

Kazuhiko Matsuda, Alastair M. Hosie, Caleb W. Holyoke, James J. Rauh, David B. Sattelle

    Research output: Contribution to journalArticlepeer-review

    Abstract

    A novel tricyclic dinitrile, KN244, blocked the wild-type (dieldrin-sensitive) homo-oligomeric γ-aminobutyric acid (GABA)-gated chloride channel of Drosophila melanogaster expressed in Xenopus oocytes. Sensitivity to the block by KN244 of the response to 30 μM GABA (IC50 = 41.6 nM, wild-type RDL(ac)) was reduced abut 100 fold (IC50 = 4.5 μM) in the dieldrin-resistant (RDL(ac)(A302S)) form of RDL.
    Original languageEnglish
    Pages (from-to)1305-1307
    Number of pages2
    JournalBritish Journal of Pharmacology
    Volume127
    Issue number6
    DOIs
    Publication statusPublished - 1999

    Keywords

    • Drosophila melanogaster
    • GABA-gated Cl- channel
    • KN244 (a tricyclic dinitrile)
    • RDL (resistant to dieldrin) subunit

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