Dr. Ron’s Research Review – October 31, 2018

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This week’s research review focuses on Phenibut.

Phenibut

Phenibut (4-amino-3-phenylbutyric acid, beta-phenyl-GABA) is a GABA derivative that easily crosses the blood/brain barrier, binds to GABA receptors, and helps increase GABA levels. Phenibut also helps inhibit the excitatory neurotransmitter phenylethylamine, while providing anti-convulsant, anti-arrhythmic, and anti-aggression effects. (Lapin, 2001)
Phenibut is thought to act as a GABA-B receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB).
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. (Lapin, 2001)
A study found that phenibut and its derivatives normalized cellular (index of delayed-type hypersensitivity reaction) and humoral (antierythrocyte antibody titer) immunity and the lymphoproliferative processes in immunocompetent organs of animals with cyclophosphamide-induced immunosuppression. This indicates pronounced immunocorrective effects of these substances. (Tyurenkov and Samotrueva, 2009)
Side effects of phenibut include sedation, sleepiness, nausea, irritability, agitation, dizziness, and headache, among others.

 

Dr. Ron


 

Articles

Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.
            (Lapin, 2001) Download
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.

Comparative study of immunocorrective activity of phenibut and its organic salts in experimental immunodeficiency.
            (Tyurenkov and Samotrueva, 2009) Download
Phenibut and its derivatives normalized cellular (index of delayed-type hypersensitivity reaction) and humoral (antierythrocyte antibody titer) immunity and the lymphoproliferative processes in immunocompetent organs of animals with cyclophosphamide-induced immunosuppression. This indicates pronounced immunocorrective effects of these substances.

 


References

Lapin, I (2001), ‘Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.’, CNS Drug Rev, 7 (4), 471-81. PubMed: 11830761
Tyurenkov, IN and MA Samotrueva (2009), ‘Comparative study of immunocorrective activity of phenibut and its organic salts in experimental immunodeficiency.’, Bull Exp Biol Med, 147 (5), 606-8. PubMed: 19907750