Pharmacological activity of optical isomers of?-phenyl-?-aminobutyric acid

Khaunina, R. A.

doi:10.1007/bf00807673

Cited by 6 publications

(8 citation statements)

References 1 publication

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“…Pharmacological effects of optical isomers of PB and PB racemate have been compared in mice (18). In all tests used (motor activity, coordination, muscle relaxation, body temperature, potentiation of barbiturates) only the d-isomer was active.…”

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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“…It is thought to act primarily on metabotropic GABA B receptors and to a lesser extent GABA A, with some experimental reports suggesting action at dopamine and other receptors (1). Commercially available phenibut typically includes racemic mixtures of both R- and S- isomers, with preclinical data indicating that the majority of pharmacological activity relies on the R- enantiomer (1, 3, 4). While the vast majority of pharmacological activity of phenibut appears to be very similar to baclofen, at least one preclinical report in mice reveals R- phenibut binding to the α2-δ subunit of voltage-dependent calcium channels, exerting gabapentin-like effects (5).…”

Section: Discussionmentioning

confidence: 99%

Dissociative Intoxication and Prolonged Withdrawal Associated With Phenibut

Joshi

Friend

Jimenez³

et al. 2017

J Clin Psychopharmacol

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Changes in body temperature after administration of amino acids, peptides, dopamine, neuroleptics and related agents: II

Clark

Lipton

1985

Neuroscience & Biobehavioral Reviews

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This survey begins a second series of compilations of data regarding changes in body temperature induced by drugs and related agents. The information listed includes the species used, the route of administration and dose of drug, the environmental temperature at which experiments were performed, the number of tests, the direction and magnitude of change in body temperature and remarks on the presence of special conditions, such as age or brain lesions. Also indicated is the influence of other drugs, such as antagonists, on the response to the primary agent. Most of the papers were published since 1978, but data from many earlier papers are also tabulated.

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Pharmacological activity of optical isomers of?-phenyl-?-aminobutyric acid

Cited by 6 publications

References 1 publication

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

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

Dissociative Intoxication and Prolonged Withdrawal Associated With Phenibut

Changes in body temperature after administration of amino acids, peptides, dopamine, neuroleptics and related agents: II

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