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Phenibut
(beta-phenyl-gamma-aminobutyric acid HCl) is a neuropsychotropic drug
that was discovered and introduced into clinical practice in Russia in
the 1960s. It has anxiolytic and nootropic (cognition enhancing)
effects. It acts as a GABA-mimetic, primarily at GABA(B) and, to some
extent, at GABA(A) receptors. It also stimulates dopamine receptors and
antagonizes beta-phenethylamine (PEA), a putative endogenous anxiogenic.
The psychopharmacological activity of phenibut is similar to that
of baclofen, a p-Cl-derivative of phenibut. This article reviews the
structure-activity relationship of phenibut and its derivatives.
Emphasis is placed on the importance of the position of the phenyl ring,
the role of the carboxyl group, and the activity of optical isomers.
Comparison of phenibut with piracetam and diazepam reveals similarities
and differences in their pharmacological and clinical effects. Phenibut
is widely used in Russia to relieve tension, anxiety, and fear, to
improve sleep in psychosomatic or neurotic patients; as well as a pre-
or post-operative medication. It is also used in the therapy of
disorders characterized by asthenia and depression, as well as in
post-traumatic stress, stuttering and vestibular disorders.
Phenibut is similar to the brain chemical called gamma-aminobutyric
acid (GABA). Research in animals shows that it might decrease anxiety
and have other effects on the body. But phenibut has not been studied in
people, so no one knows whether it might work as a medicine.
