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XB-ART-54624
Chemistry 2017 Aug 10;2345:10848-10852. doi: 10.1002/chem.201701443.
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The Synthesis and Evaluation of Fluoro-, Trifluoromethyl-, and Iodomuscimols as GABA Agonists.

Abdul Manan MAF , Cordes DB , Slawin AMZ , Bühl M , Liao VWY , Chua HC , Chebib M , O'Hagan D .


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Halogenated analogues of the neurotoxic alkaloid muscimol were prepared with fluorine, iodine or trifluoromethyl at the 4 position of the isoxazole ring system. These compounds were investigated as agonists for GABA A receptors. Only the C-4 fluorine-containing analogue proved to be an active compound in these assays. The fluoro analogue was less active than muscimol, however it showed differential activity between synaptic (α 1 β 2 γ 2 ) and extrasynaptic (α 4 β 2 γ) GABA A receptors, having a similar potency to the neurotransmitter GABA for the extrasynaptic (α 4 β 2 γ) receptor.

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