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

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.

British Journal of Pharmacology (1999) 127, 1305–1307; doi:10.1038/sj.bjp.0702663

DOI: 10.1038/sj.bjp.0702663

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