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.
MeSH terms
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Animals
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Bridged Bicyclo Compounds / pharmacology*
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Chloride Channels / antagonists & inhibitors
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Dieldrin / pharmacology*
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Dose-Response Relationship, Drug
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Drosophila melanogaster
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GABA Antagonists / pharmacology*
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Insecticide Resistance
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Insecticides / pharmacology*
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Membrane Potentials / drug effects
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Nitriles / pharmacology*
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Oocytes / drug effects
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Oocytes / physiology
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Receptors, GABA / drug effects*
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Xenopus
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gamma-Aminobutyric Acid / pharmacology
Substances
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Bridged Bicyclo Compounds
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Chloride Channels
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GABA Antagonists
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Insecticides
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KN 244
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Nitriles
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Receptors, GABA
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gamma-Aminobutyric Acid
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Dieldrin