1. The Synthesis and Evaluation of Fluoro-, Trifluoromethyl-, and Iodomuscimols as GABA Agonists.
- Author
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Abdul Manan MAF, Cordes DB, Slawin AMZ, Bühl M, Liao VWY, Chua HC, Chebib M, and O'Hagan D
- Subjects
- Animals, Crystallography, X-Ray, GABA Agonists chemical synthesis, GABA Agonists metabolism, Molecular Conformation, Muscimol chemical synthesis, Muscimol metabolism, Oocytes metabolism, Receptors, GABA-A genetics, Receptors, GABA-A metabolism, Xenopus laevis growth & development, Xenopus laevis metabolism, Fluorine chemistry, GABA Agonists chemistry, Muscimol chemistry
- 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 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 (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., (© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)- Published
- 2017
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