Abstract
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 GABAA 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 (α1 β2 γ2 ) and extrasynaptic (α4 β2 γ) GABAA receptors, having a similar potency to the neurotransmitter GABA for the extrasynaptic (α4 β2 γ) receptor.
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