Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist.
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ABSTRACT: A novel tricyclic dinitrile, KN244, blocked the wild-type (dieldrin-sensitive) homo-oligomeric gamma-aminobutyric acid (GABA)-gated chloride channel of Drosophila melanogaster expressed in Xenopus oocytes. Sensitivity to the block by KN244 of the response to 30 microM GABA (IC50=41.6 nM, wild-type RDLac) was reduced abut 100 fold (IC50=4.5 microM) in the dieldrin-resistant (RDLacA302S) form of RDL.
SUBMITTER: Matsuda K
PROVIDER: S-EPMC1760657 | biostudies-other | 1999 Jul
REPOSITORIES: biostudies-other
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