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Phenibut (beta-Phenyl-GABA): A Tranquilizer and Nootropic Drug

Phenibut (beta-Phenyl-GABA): A Tranquilizer and Nootropic Drug

  1. Gradient
    Izyaslav Lapin

    Phenibut (ß-phenyl-gamma-aminobutyric acid HCl) is a neuropsychotropic drug that was dis- covered 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 GABAB and, to some extent, at GABAA receptors. It also stimulates dopamine receptors and antag- onizes â-phenethylamine (PEA), a putative endogenous anxiogenic. The psychopharma- cological 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. Em- phasis is placed on the importance of the position of the phenyl ring, the role of the car- boxyl group, and the activity of optical isomers. Comparison of phenibut with piracetam and diazepam reveals similarities and differences in their pharmacological and clinical ef- fects. 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.
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