Like the natural occurring neurotransmitter
GABA (amino acid), it bonds to the
GABA-B metabotropic
receptor, and provides a calming action like the natural occurring neurotransmitter, and similar to other GABA agonists.
There is dispute in the literature about whether or not Phenibut binds to the GABA-A ionotropic receptor, which is responsible for the actions of benzodiazepines, barbiturates, z-drugs, and for some of the effects of ethanol.