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Published on: August 16, 2018
Muscimol as an ionotropic GABA receptor agonist
1Adrien Albert Laboratory of Medicinal Chemistry, School of Medical Sciences (Pharmacology), The University of Sydney, Sydney, NSW, 2006, Australia, grahamj@mail.usyd.edu.au.
Abstract:
Muscimol, a psychoactive isoxazole from Amanita muscaria and related mushrooms, has proved to be a remarkably selective agonist at ionotropic receptors for the inhibitory neurotransmitter GABA. This historic overview highlights the discovery and development of muscimol and related compounds as a GABA agonist by Danish and Australian neurochemists. Muscimol is widely used as a ligand to probe GABA receptors and was the lead compound in the development of a range of GABAergic agents including nipecotic acid, tiagabine, 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol, (Gaboxadol(®)) and 4-PIOL.
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