The synthesis and evaluation of fluoro-, trifluoromethyl, and iodomuscimols as GABA agonists
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 (α1β2γ2) and extrasynaptic (α4β2γ) GABAA receptors, having a similar potency to the neurotransmitter GABA for the extrasynaptic (α4β2γ) receptor.
Citation
Abdul Manan , M A F , Cordes , D , Slawin , A , Buehl , M , Liao , V , Chua , H , Chebib , M & O'Hagan , D 2017 , ' The synthesis and evaluation of fluoro-, trifluoromethyl, and iodomuscimols as GABA agonists ' , Chemistry - A European Journal , vol. 23 , no. 45 , pp. 10848-10852 . https://doi.org/10.1002/chem.201701443
Publication
Chemistry - A European Journal
Status
Peer reviewed
ISSN
0947-6539Type
Journal article
Description
MAFAM acknowledges the Ministry of Education of Malaysia and Universiti Teknologi MARA for a scholarship. MC acknowledges the funding support of the Australian National Health and Medical Research Council (APP1081733).Collections
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