| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Phenibut targets GABA-B receptors and voltage-dependent calcium channels. It is a GABA-B receptor agonist, mimicking the inhibitory neurotransmitter GABA. It also blocks voltage-dependent calcium channels, particularly the α2-δ subunit, which contributes to its anxiolytic and analgesic effects. Its mechanism of action is similar to that of baclofen.
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| ln Vitro |
Phenibut is a neuropsychiatric drug. Additionally, phenibut inhibits beta-phenylethylamine (PEA), a possible endogenous anxiolytic drug, and activates dopamine receptors [2].
Phenibut demonstrates GABA-B receptor agonist activity in vitro. It binds to GABA-B receptors with moderate affinity. It also blocks voltage-dependent calcium channels. Its activity is assessed in radioligand binding assays and functional assays measuring receptor-mediated signaling (e.g., inhibition of cAMP accumulation). Its IC50 or Ki values for GABA-B receptors are available in the literature. |
| ln Vivo |
Phenibut is used clinically as an anxiolytic, sedative, and nootropic agent. It is approved for the treatment of anxiety, insomnia, and post-traumatic stress disorder in Russia and several other countries. It has also been used to treat alcohol withdrawal syndrome and stuttering. Its anxiolytic effects are comparable to those of benzodiazepines but with a different mechanism of action.
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| Enzyme Assay |
GABA-B receptor binding assays are performed using membranes prepared from rat brain or from cells expressing recombinant GABA-B receptors. Radioligand binding studies use [3H]-baclofen or [3H]-GABA as labeled ligands. Membrane preparations are incubated with varying concentrations of Phenibut and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 2.5 mM CaCl2) for 60 minutes at room temperature. Non-specific binding is determined using excess baclofen. Bound radioactivity is measured by scintillation counting after filtration. IC50 and Ki values are calculated by non-linear regression.
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| Cell Assay |
Cellular GABA-B receptor activation is evaluated in cell lines expressing recombinant GABA-B receptors (e.g., HEK-293 cells co-expressing GABA-B1 and GABA-B2). Cells are cultured in appropriate media and treated with Phenibut at various concentrations. Functional assays measure receptor-mediated inhibition of cAMP accumulation (Gi-coupled receptor). The compound's agonist activity is assessed by its ability to inhibit forskolin-stimulated cAMP production. Cell viability is assessed using MTT or LDH assays. Each experiment includes known GABA-B agonists (baclofen) as positive controls.
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| Animal Protocol |
In vivo studies are conducted in animal models of anxiety (elevated plus maze, open field test), insomnia, and seizure. Phenibut is administered orally or intraperitoneally at doses determined by preclinical studies. Anxiolytic effects are assessed by increased time in open arms of the elevated plus maze. Sedative effects are assessed by locomotor activity. Clinical studies have been conducted for anxiety, insomnia, and PTSD.
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| ADME/Pharmacokinetics |
Phenibut has a molecular weight of 179.22 g/mol and a molecular formula of C10H13NO2. IUPAC name: 4-amino-3-phenylbutanoic acid. Appearance: white crystalline powder. Solubility: soluble in water. Storage: typically at room temperature. As a clinically used drug, its pharmacokinetics are well-characterized: it is absorbed from the gastrointestinal tract, reaches peak plasma levels in 1-2 hours, and has a half-life of approximately 5 hours. It is excreted renally.
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| Toxicity/Toxicokinetics |
Phenibut is generally well-tolerated at therapeutic doses. Common adverse effects may include drowsiness, dizziness, nausea, and headache. At higher doses, it can cause sedation, ataxia, and respiratory depression. Tolerance and dependence can develop with prolonged use. Withdrawal symptoms may occur upon discontinuation. It is contraindicated in patients with hypersensitivity and in pregnant women.
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| References | |
| Additional Infomation |
Phenibut is a nitrogen- and oxygen-containing organic compound whose function is related to γ-amino acids.
Phenibut is also known as β-phenyl-γ-aminobutyric acid, Fenibut, and Noofen. It is a central nervous system depressant with anxiolytic and nootropic effects. It is approved for clinical use in Russia and several other countries for anxiety, insomnia, and PTSD. It is available as a prescription drug in some countries and as a dietary supplement in others. |
| Molecular Formula |
C10H13NO2
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| Molecular Weight |
179.219
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| Exact Mass |
215.071
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| CAS # |
1078-21-3
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| Related CAS # |
Phenibut hydrochloride;3060-41-1
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| PubChem CID |
14113
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| Appearance |
Typically exists as solid at room temperature
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| Melting Point |
194.0-202.0°C
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| LogP |
2.705
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
164
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CC(CN)C1C=CC=CC=1)=O
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| InChi Key |
DAFOCGYVTAOKAJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13NO2/c11-7-9(6-10(12)13)8-4-2-1-3-5-8/h1-5,9H,6-7,11H2,(H,12,13)
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| Chemical Name |
4-amino-3-phenylbutanoic acid
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| Synonyms |
Fenigam; Fenibut; Phenibut
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 0.5580 mL | 2.7899 mL | 5.5797 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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