Tranquilizing effects of ?-phenyl-?-aminobutyric acid (phenygam)

Khaunina, R. A.

doi:10.1007/bf00783474

Cited by 7 publications

(5 citation statements)

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“…Unlike GABA, PB completely lacks anticonvulsant activity by either systemic or intracerebroventricular (i.c.v.) administration (16,20,25,32,37,38). The lack of anticonvulsant activity of PB may be related to the reduction in norepinephrine-independent [ 3 H]GABA binding to brain synaptic membranes by â-substituted GABA derivatives.…”

Section: Structure-activity Relationshipsmentioning

confidence: 99%

“…1). Therefore, most of the pharmacological studies with PB were devoted to its GABA-like properties, its effects on GABA receptors and to comparison with other GABAergic compounds (1)(2)(3)5,6,9,11,(16)(17)(18)(19)(20)(21)(22)(23)32,43,(47)(48)(49)(50). PB can be viewed, however, also as a derivative of PEA (Fig.…”

Section: Putative Mechanisms Of the Central Action Of Pbmentioning

confidence: 99%

“…1) was synthesized by Perekalin and his associates at the Department of Organic Chemistry of the Herzen Pedagogic Institute in St. Petersburg, Russia. In initial publications (16)(17)(18)36,37) phenibut was known as phenigamma.…”

Section: Introductionmentioning

confidence: 99%

“…The pharmacological properties of PB were evaluated by Khaunina and her associates (16)(17)(18)20,45). The in vitro neuronal effects of PB and related GABA derivatives were studied on isolated cat cerebral neurons (10,11).…”

Section: Introductionmentioning

confidence: 99%

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Phenibut (β‐Phenyl‐GABA): A Tranquilizer and Nootropic Drug

2001

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Phenibut (â-phenyl-ã-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 â-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.

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Section: Structure-activity Relationshipsmentioning

confidence: 99%

Section: Putative Mechanisms Of the Central Action Of Pbmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Phenibut (β‐Phenyl‐GABA): A Tranquilizer and Nootropic Drug

2001

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show abstract

“…Phenibut was first created by Perekalin and his associates at the Department of Organic Chemistry of the Herzen Pedagogic Institute in St. Petersburg, Russia (Lapin, 2001). It was originally known as 'phenigamma' (Khaunma, 1964;1968;1971;Maslova & Khaunina, 1965;1967). It was synthesised as an organic derivative of GABA, with an extra phenyl ring attached to its second carbon (Lapin, 2001;Li & Sundararajan, 2015).…”

Section: Pharmacology and Clinical Use Of Phenybutmentioning

confidence: 99%