GABAA 3 Activators

GABAA receptor subunit alpha-3 Activators comprise a diverse group of chemical compounds that facilitate the receptor's function by enhancing the GABAergic inhibitory neurotransmission. Allopregnanolone, for example, significantly prolongs the opening of the GABAA receptor chloride channel, thus potentiating the inhibitory effect of GABA itself and directly amplifying the activity of the GABAA receptor subunit alpha-3. Similarly, compounds like Zolpidem exhibit a preferential binding to receptors containing the alpha-3 subunit, selectively augmenting the inhibitory action of GABA and by extension, the activity of GABAA receptor subunit alpha-3.

Benzodiazepines and Barbiturates, although binding to distinct sites, have a synergistic effect in enhancing GABA's affinity to its receptor or prolonging the open state of the chloride channel, respectively, leading to an indirect but definite upregulation of the GABAA receptor subunit alpha-3 function. Furthermore, anesthetics like Propofol and Etomidate enhance GABAA receptor-mediated currents, contributing to the greater efficacy of GABS.