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A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1]
It is made from pregnenolone, and is a positive allosteric modulator of the action of γ-aminobutyric acid (GABA) at GABA A receptor. [10] Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA action at GABA A receptor such as the benzodiazepines, including anxiolytic, sedative, and anticonvulsant ...
At GABA A receptors etifoxine binds at the α+β− interface and preferentially potentiates α 2 β 3 γ 2 and α 3 β 3 γ 2 receptor types. [25] This direct allosteric potentiation can only be observed at relatively high concentrations (starting at >1 mM) and is perhaps not physiologically relevant at normal human doses. [ 26 ]
The therapeutic as well as adverse effects of midazolam are due to its effects on the GABA A receptors; midazolam does not activate GABA A receptors directly but, as with other benzodiazepines, it enhances the effect of the endogenous neurotransmitter GABA on the GABA A receptors (increasing the frequency of Cl − channel opening) resulting in ...
[9] [10] [11] The inhibitory neurotransmitter GABA plays a complex role in modulating anxiety and stress, regulating sleep, circadian rhythms, mood, cognition, and perception. Low GABA levels are associated with emotional and behavioral disruptions, including short-term and/or long-term stress, anxiety disorders, and sleep disorders. [12]
Gaboxadol is a supra-maximal agonist at α 4 β 3 δ, low-potency agonist at α 1 β 3 γ 2, partial agonist at α 4 β 3 γ, and antagonist at ρ1 GABA A receptors. [5] [6] [7] Its affinity for extrasynaptic α 4 β 3 δ GABA A receptors is 10-fold greater than other subtypes. [8]