Abstract
Modification of the major insecticide fipronil (1) by replacing three pyrazole substituents (hydrogen for both cyano and amino and trifluoromethyldiazirinyl for trifluoromethylsulfinyl) gives a candidate photoaffinity probe (3) of high potency (IC(50) 2-28 nM) in blocking the chloride channel of Drosophila and human beta 3 GABA receptors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Dose-Response Relationship, Drug
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Drosophila
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Humans
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Insecticides / pharmacology*
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Photoaffinity Labels / metabolism
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry*
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Pyrazoles / metabolism
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Pyrazoles / pharmacology*
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Receptors, GABA-B / drug effects*
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gamma-Aminobutyric Acid / pharmacology
Substances
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Insecticides
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Photoaffinity Labels
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Pyrazoles
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Receptors, GABA-B
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gamma-Aminobutyric Acid
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fipronil