Phenibut
GABA-B Agonist | Anxiolytic & Sleep Aid
Phenibut (beta-phenyl-gamma-aminobutyric acid) is a synthetic GABA analog developed in the Soviet Union in the 1960s. It was designed to cross the blood-brain barrier, which GABA itself cannot do efficiently, by adding a phenyl ring to the GABA molecule. Phenibut has been prescribed in Russia and several former Soviet states since the 1960s for the treatment of anxiety, insomnia, post-traumatic stress disorder, vestibular disorders, and stuttering. It was famously included in the medical kit of Soviet cosmonauts for its calming effects without impairing cognitive performance. Phenibut is NOT approved by the FDA, EMA, or any Western regulatory agency as a pharmaceutical drug. In the United States, Australia, and parts of Europe, it has been sold as a dietary supplement or nootropic, though several countries have moved to restrict or ban its sale due to growing reports of dependence, withdrawal, and adverse events. The addiction and dependence potential of phenibut is HIGH, and tolerance develops rapidly with repeated use. This compound should be treated with the same caution as benzodiazepines or other GABAergic drugs.
Moleküler Gösterim
M.W.: 179.22 Da
PubChem 2D yapı diyagramı
Referans Flakon
Referans illüstrasyonu — ürün listesi değildir
Etki Mekanizması
Phenibut acts primarily as an agonist at GABA-B receptors, the same receptor target as baclofen (to which it is structurally related). GABA-B receptor activation inhibits neuronal excitability by opening potassium channels and reducing calcium influx at presynaptic terminals, leading to decreased neurotransmitter release and a net inhibitory effect on the central nervous system. This produces anxiolytic, sedative, and muscle-relaxant effects. In addition to GABA-B agonism, phenibut blocks voltage-dependent calcium channels (VDCCs), particularly alpha-2-delta subunit-containing channels, a mechanism shared with gabapentin and pregabalin. This contributes to its anxiolytic and analgesic properties. At higher doses, phenibut may also weakly stimulate GABA-A receptors, contributing to its sedative effects, though this is not its primary mechanism at typical doses. The R-enantiomer of phenibut is responsible for the majority of its GABA-B receptor activity, while the S-enantiomer is more selective for the alpha-2-delta VDCC subunit.
Phenibut (beta-phenyl-gamma-aminobutyric acid) is a synthetic GABA analog developed in the Soviet Union in the 1960s. It was designed to cross the blood-brain barrier, which GABA itself cannot do efficiently, by adding a phenyl ring to the GABA molecule. Phenibut has been prescribed in Russia and several former Soviet states since the 1960s for the treatment of anxiety, insomnia, post-traumatic stress disorder, vestibular disorders, and stuttering. It was famously included in the medical kit of Soviet cosmonauts for its calming effects without impairing cognitive performance. Phenibut is NOT approved by the FDA, EMA, or any Western regulatory agency as a pharmaceutical drug. In the United States, Australia, and parts of Europe, it has been sold as a dietary supplement or nootropic, though several countries have moved to restrict or ban its sale due to growing reports of dependence, withdrawal, and adverse events. The addiction and dependence potential of phenibut is HIGH, and tolerance develops rapidly with repeated use. This compound should be treated with the same caution as benzodiazepines or other GABAergic drugs.
Moleküler Veri
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Doz Protokolleri
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| Hedef | Doz | Sıklık | Yol |
|---|---|---|---|
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Etkileşimler
Alcohol
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Kaynaklar
- Phenibut (beta-Phenyl-GABA): A Tranquilizer and Nootropic Drug — Lapin, I.
- Phenibut Dependence: A Case Report and Literature Review — Samokhvalov, A.V., Paton-Gay, C.L., Balchand, K., Rehm, J.
- Phenibut (4-Amino-3-Phenyl-Butyric Acid): Availability, Prevalence of Use, Desired Effects and Acute Toxicity — Owen, D.R., Wood, D.M., Archer, J.R., Dargan, P.I.
- Baclofen and Phenibut: Comparison of GABA-B Receptor Binding and Neurochemical Effects — Dambrova, M., Zvejniece, L., Liepinsh, E., et al.
- Phenibut Addiction and Withdrawal: Clinical Presentation and Treatment — Ahuja, T., Mgbako, O., Katzman, C., Grossman, A.