Phenibut(Synonyms: 菲尼布特,β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid) 目录号 : GC63146
An Analytical Reference Standard
Sample solution is provided at 25 µL, 10mM.
Phenibut (hydrochloride) is an analytical reference standard categorized as a gabapentinoid and a nootropic.1,2 Phenibut also has sedative properties.3 This product is intended for research and forensic applications.
1.Bowery, N.G., Hill, D.R., and Hudson, A.L.Characteristics of GABAB receptor binding sites on rat whole brain synaptic membranesBr. J. Pharmacol.78(1)191-206(1983) 2.Tyurenkov, I.N., Borodkina, L.E., Bagmetova, V.V., et al.Comparison of nootropic and neuroprotective features of aryl-substituted analogs of gamma-aminobutyric acidBull. Exp. Biol. Med.160(4)465-469(2016) 3.Lapin, I.Phenibut (β-phenyl-GABA): a tranquilizer and nootropic drugCNS Drug Rev.7(4)471-481(2001)
|别名||菲尼布特,β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid|
|溶解度||储存条件||Store at -20°C|
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
|1 mg||5 mg||10 mg|
|1 mM||5.5797 mL||27.8987 mL||55.7973 mL|
|5 mM||1.1159 mL||5.5797 mL||11.1595 mL|
|10 mM||0.558 mL||2.7899 mL||5.5797 mL|
|% DMSO % % Tween 80 % saline|
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug
CNS Drug Rev 2001 Winter;7(4):471-81.PMID:11830761DOI:10.1111/j.1527-3458.2001.tb00211.x.
Phenibut (beta-phenyl-gamma-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 beta-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.
Phenibut (β-Phenyl-γ-Aminobutyric Acid): an Easily Obtainable "Dietary Supplement" With Propensities for Physical Dependence and Addiction
Curr Psychiatry Rep 2019 Mar 9;21(4):23.PMID:30852710DOI:10.1007/s11920-019-1009-0.
Purpose of review: Phenibut (β-phenyl-γ-aminobutyric acid) is a psychoactive GABA analogue currently being marketed online as an anxiolytic and nootropic dietary supplement. Its use is growing in popularity, but its pharmacological activity is well beyond that of a conventional nutritional supplement, and similar to that of a prescription strength sedative. This review will focus on the potential adversities of Phenibut use and will discuss what treatment options may be beneficial to afflicted patients. Recent findings: Over the last several years, multiple case reports have highlighted Phenibut's potential to produce the conditions of physical dependence, withdrawal, and addiction. In cases involving intoxication, patients have presented with a varying degree of mental status changes, from being minimally responsive to manifesting symptoms of an agitated delirium. Phenibut is a potent psychoactive substance with GABAB agonist properties, which is emerging as a drug of misuse through growing internet sales. Its marketing as a "dietary supplement" is inaccurate and misleading, given its pharmacological profile and ability to induce the physiological changes associated with withdrawal and physical dependence.
BMJ Case Rep 2013 Feb 6;2013:bcr2012008381.PMID:23391959DOI:10.1136/bcr-2012-008381.
Phenibut is a γ-aminobutyric acid (GABA) agonist designed and used as an anxiolytic in Russia. In Western countries, Phenibut is not a registered medication but is available through online stores as a supplement. We present a case of a patient who used Phenibut to self-medicate anxiety, insomnia and cravings for alcohol. While Phenibut was helpful initially, the patient developed dependence including tolerance, significant withdrawal symptoms within 3-4 h of last use and failure to fulfil his roles at work and at home. He finally sought medical assistance in our addictions clinic. We have gradually, over the course of 9 weeks, substituted Phenibut with baclofen, which has similar pharmacological properties, and then successfully tapered the patient off baclofen. This required approximately 10 mg of baclofen for each gram of Phenibut.
Quantity of Phenibut in dietary supplements before and after FDA warnings
Clin Toxicol (Phila) 2022 Apr;60(4):486-488.PMID:34550038DOI:10.1080/15563650.2021.1973020.
Introduction: Phenibut is used to treat anxiety, insomnia, alcohol withdrawal and other conditions in Russia. The drug, however, has abuse potential and may cause lethargy, delirium, psychosis and coma. In the United States (US), the US Food and Drug Administration (FDA) has never approved the use of Phenibut as a prescription medication, but the drug is available over-the-counter in dietary supplements. More than 80 cases of coma and death have been associated with Phenibut consumption and withdrawal, and the FDA recently warned that the drug is not permitted in over-the-counter supplements. We designed our study to determine the presence and quantity of Phenibut in over-the-counter supplements before and after the FDA warnings. Methods: Phenibut products were included if they (a) listed Phenibut or a synonym as an ingredient on the label, (b) were labeled as a dietary supplement, and (c) were available for sale both before and after the FDA warning. Supplements were analyzed by liquid chromatography time-of-flight mass spectrometry; quantification was performed by isotope dilution method. Results: Four brands of dietary supplements labeled as containing Phenibut met the inclusion criteria. Prior to the FDA warnings, two of the four brands contained Phenibut, at dosages of 484 mg and 487 mg per serving. After the FDA warning, all four products contained Phenibut, ranging in dosages from 21 mg to 1,164 mg per serving. Phenibut was first detected only after the FDA warnings in two brands, and the quantity of Phenibut increased in three of four products after the FDA warnings. Quantities detected per dose were as much as 450% greater than a typical 250 mg pharmaceutical tablet manufactured in Russia. Conclusion: Following FDA issuing an advisory that Phenibut is not permitted in dietary supplements, the quantity of Phenibut increased in 3 of 4 brands of over-the-counter Phenibut supplements.
Acute Phenibut withdrawal: A comprehensive literature review and illustrative case report
Bosn J Basic Med Sci 2019 May 20;19(2):125-129.PMID:30501608DOI:10.17305/bjbms.2018.4008.
Phenibut is a glutamic acid derivative with activity on the γ-aminobutyric acid (GABA)B, A, and B-phenethylamine receptors. It is prescribed in former Communist Bloc countries for anxiolysis and related psychiatric disorders. It can be easily obtained in Western countries and is thought to have abuse potential. Abrupt discontinuation has been reported to precipitate an abstinence syndrome. A review of the literature identified 22 reported cases, many of which were notable for severe psychomotor agitation and requirements for aggressive pharmacologic treatment. Neurologic and autonomic signs and symptoms may mimic serotonin or neuroleptic malignant syndrome. Patients were typically younger and had coexisting substance abuse disorders to other drugs. Also presented is a case of a 23-year-old male with an acute Phenibut abstinence syndrome. This patient exhibited severe psychomotor agitation requiring physical restraints, dexmedetomidine, lorazepam, haloperidol, diphenhydramine, cyproheptadine, melatonin, olanzapine, and baclofen for symptom control.