Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …

Abstract γ-Aminobutyric acid type A (GABAA) receptors mediate fast inhibitory signaling in
the brain and are targets of numerous drugs and endogenous neurosteroids. A subset of …

Lipids modulate the function of many ion channels, possibly through direct lipid-protein
interactions. The recent outpouring of ion channel structures by cryo-EM has revealed many …

This study examines how site-specific binding to three identified neurosteroid-binding sites
in the α1β3 GABAA receptor (GABAAR) contributes to neurosteroid allosteric modulation …

Ligand-gated ion channels are integral membrane proteins that activate through a change in
conformation upon transmitter binding and were identified as key players of brain function …

The neurosteroid allopregnanolone (ALLO) and pregnanolone (PREG), are equally effective
positive allosteric modulators (PAMs) of GABAA receptors. Interestingly, the PAM effects of …

Since the 1990s, there has been waning interest in researching general anaesthetics
(anaesthetics). Although currently used anaesthetics are mostly safe and effective, they are …

Brain inhibition is a vital process for controlling and sculpting the excitability of the central
nervous system in healthy individuals. This level of control is provided over several …

The recent approval of formulations of the endogenous neurosteroid allopregnanolone
(brexanolone) and the synthetic neuroactive steroid SAGE-217 (zuranolone) to treat …

Neurosteroids are endogenous modulators of GABA A receptors that mediate anxiety, pain,
mood and arousal. The 3-hydroxyl epimers, allopregnanolone (3α-OH) and epi …