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Phenibut GABA Receptor agonist

Name: Phenibut
Brand: Selleck Chemicals
SKU: S4892
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4892

Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.

Chemical Structure

Molecular Weight: 179.22

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.04%

99.04

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor TRP Channel GluR MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Serotonin Transporter Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor
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Chemical Information, Storage & Stability

Molecular Weight	179.22	Formula	C₁₀H₁₃NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1078-21-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Aminophenylbutyric acid, Fenibut, Fenigam, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA			Smiles	C1=CC=C(C=C1)C(CC(=O)O)CN

Solubility

In vitro
Batch:

DMSO : 36 mg/mL (200.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 36 mg/mL

Ethanol : 36 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.8mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 36 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.26mg/ml (1.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	GABA receptor ^[1]
In vitro	Phenibut has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABAB and, to some extent, at GABAA receptors. This compound also stimulates dopamine receptors and antagonizes β-phenethylamine (PEA), a putative endogenous anxiogenic^[1].
In vivo	At doses that do not affect motor activity (e.g., 20 mg/kg i.p.), Phenibut inhibits food conditioned reflexes in mice. At doses higher than 70 mg/kg i.p., this compound reduces motor and exploratory activities, rearings, muscle tone, coordination and body temperature. Following intravenous administration to either rabbits or rats it is not metabolized. This chemical is largely excreted in the urine. At 15, 30, 60, or 90 min following i.v. administration it is found in liver, kidneys, and urine. Traces of the compound are found in blood and brain. 180 min after i.v. injection only traces of the drug are found in all tissues studied. In cats and dogs, it, after a single dose of 50 mg/kg i.v., is excreted in the urine unchanged. The acute toxicity of this substance is low. Its LD50 is 900 mg/kg i.p. in mice and 700 mg/kg i.p. in rats^[1]. Administration of this agent leads to decreases in horizontal movement activity and some elements of investigative behavior in rabbits in the open field, along with decreases in the reactivity of the animals to emotionally significant stimuli^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/11830761/ [2] https://pubmed.ncbi.nlm.nih.gov/18607733/

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