DUAL MECHANISM OF ACTION
GRX-917 has a dual mechanism of action: A) it works at GABA channels, and B) it increases neurosteroids.
A) Direct actions at GABA Channels
Increased action at GABA channels slows excess neuronal excitation, easing anxiety symptoms. Nonselective, over activation of GABA channels, however, can lead to sedation and other undesired effects. GRX-917 and etifoxine increase activation only at selected subset of GABA channels (channels with β2/3 subunits (Figure A).
Drugs like alcohol, barbiturates, benzodiazepines and Propofol, also work at GABA, but increase action at GABA channels nonselectively, causing sedation and potentially dangerous side effects.
Scientific Explanation: GRX-917 boosts GABAergic transmission via preferential positive allosteric modulation (PAM) of β2/3-subunit-containing GABA receptors, at a binding site distinct from benzodiazepines.