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Sirisoma NS, Ratra GS, Tomizawa M, Casida JE: Fipronil-based photoaffinity probe for Drosophila and human beta 3 GABA receptors. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2979-81.
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. |
81(1,1,1,1) |