Distribution of?-phenyl-?-aminobutyric acid (phenygam) in the organism and cartain indices of its central effects

Маслова, М. Н.; Khaunina, R. A.

doi:10.1007/bf00805044

Cited by 4 publications

(5 citation statements)

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“…or i.p., produced slow amplitude spikes in the EEG. The spikes appeared 15 to 30 min after administration of the drug and lasted for 2 h. On the next day the EEG was normal (36). The primary effects of PB, unlike those of GABA, were subcortical.…”

Section: General Neuropsychopharmacological Effectsmentioning

confidence: 94%

“…Incorporation of a phenyl ring into the GABA molecule was expected to improve the entry of the molecule into the brain. Following incorporation, Maslova and Khaunina (36,37) demonstrated that in mice and rats PB penetrates the blood-brain barrier significantly better than GABA. Subsequently, Davies and Watkins (11) studied the effects of â-phenyl derivatives of GABA on chemically induced firing of isolated cat cerebral neurons.…”

Section: Structure-activity Relationshipsmentioning

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%

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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: General Neuropsychopharmacological Effectsmentioning

confidence: 94%

Section: Structure-activity Relationshipsmentioning

confidence: 99%

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

2001

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“…The phenyl ring enhances the entry of the drug into the brain. 19,20 Phenibut is a racemic mixture of the R-phenibut and S-phenibut enantiomers, with the R-enantiomer being the most pharmacologically active of the 2. [21][22][23] The pharmacologic effects of phenibut largely center on its role as a GABA B receptor agonist, similar to the structurally related compound β-(4-chlorophenyl)-GABA (baclofen), which differs from phenibut by a p-choro group (Figure 1).…”

Section: Chemical Structure and Mechanism Of Action (Moa)mentioning

confidence: 99%

“…The molecular structure of phenibut is characterized by the assimilation of a phenyl ring at the β ‐position into the γ ‐aminobutyric acid (GABA) molecule (Figure 1). The phenyl ring enhances the entry of the drug into the brain 19,20 . Phenibut is a racemic mixture of the R‐phenibut and S‐phenibut enantiomers, with the R‐enantiomer being the most pharmacologically active of the 2 21–23 .…”

Section: Pharmacologymentioning

confidence: 99%

Phenibut: Review and Pharmacologic Approaches to Treating Withdrawal

Penzak,

Bulloch

2024

The Journal of Clinical Pharma

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Abstractβ‐Phenyl‐γ‐aminobutyric acid (phenibut) is an analog of the inhibitory neurotransmitter γ‐aminobutyric acid (GABA) that was first synthesized in Russia in the early 1960s. It is marketed as a nootropic (smart drug) to improve cognitive performance, and to treat generalized and social anxiety, insomnia, and alcohol withdrawal. The use of phenibut is legal in the USA and it is widely available online without a prescription. Increased public awareness of phenibut has led to a growing number of reports of acute intoxication and withdrawal. In this review, we describe the pharmacology of phenibut, the presentation and management of acute intoxication, and regulatory issues, placing particular emphasis on the treatment of acute withdrawal, for which there are no comparative studies. Among 29 cases of phenibut withdrawal, patients were successfully treated with baclofen, benzodiazepines, and phenobarbital, as individual agents or in various combinations. Ancillary medications included antipsychotics, dexmedetomidine, gabapentin, and pregabalin. After stabilization, a number of patients did well on baclofen tapers, whereas others were weaned off benzodiazepines or phenobarbital. Phenobarbital may be preferred over baclofen, or used as an added agent, in patients at risk for seizures. As long as phenibut remains legal, cases of phenibut intoxication and withdrawal are likely to increase. As urine or plasma drug screening for phenibut is not widely available, it is vital that clinicians obtain a detailed medication history in patients presenting to the emergency department with nonspecific symptoms that may represent phenibut intoxication or withdrawal. Further, clinicians may wish to consult an addiction specialist or toxicologist in these situations.

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Chapter 1. Antipsychotic and Anti-anxiety Agents

Childress¹

1966

Annual Reports in Medicinal Chemistry

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Distribution of?-phenyl-?-aminobutyric acid (phenygam) in the organism and cartain indices of its central effects

Cited by 4 publications

References 0 publications

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

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

Phenibut: Review and Pharmacologic Approaches to Treating Withdrawal

Chapter 1. Antipsychotic and Anti-anxiety Agents

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