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Drug intelligence / Profile preview
Gaboxadol is a small molecule experimental drug that acts as a highly selective agonist at extrasynaptic GABAA receptors containing the α4 and δ subunits. Unlike benzodiazepines and other sedative-hypnotics that act primarily at synaptic GABAA receptors, gaboxadol targets delta-containing GABAA receptor subtypes located outside the synapse (extrasynaptic), particularly those with α4β3δ composition. This mechanism enhances tonic inhibition in the brain and is thought to promote slow-wave sleep by modulating thalamic neuronal activity. Gaboxadol was originally developed as a sleep aid for insomnia by Lundbeck and Merck but its development was discontinued in 2007 due to concerns about safety and efficacy. More recently, it has been investigated for neurological disorders such as Angelman syndrome, fragile X syndrome, and epilepsy[1][2][3][4][5].
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