Phenibut | CAS#1078-21-3 | GABA analogue

Phenibut
featured

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 584435

CAS#: 1078-21-3

Description: Phenibut, a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.

Chemical Structure

Phenibut

CAS# 1078-21-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 584435
Name: Phenibut
CAS#: 1078-21-3
Chemical Formula: C10H13NO2
Exact Mass: 179.09
Molecular Weight: 179.219
Elemental Analysis: C, 67.02; H, 7.31; N, 7.82; O, 17.85

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 280
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Phenibut; Fenibut; Fenigam; Phenigam; Phenybut; PhGABA

IUPAC/Chemical Name: 4-Amino-3-phenylbutyric acid

InChi Key: DAFOCGYVTAOKAJ-UHFFFAOYSA-N

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)

SMILES Code: O=C(O)CC(C1=CC=CC=C1)CN

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Phenibut, a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
In vitro activity:	The present study compared the potency of F-phenibut, phenibut, and the GABAB agonist (±)-baclofen (baclofen) using in vitro patch-clamp recordings obtained from mouse cerebellar Purkinje cells slice preparations. These findings indicate that F-phenibut acted as a potent GABAB agonist. EC50 of outward current density evoked by the three GABAB agonists decreased in the following order: phenibut (1362 μM) > F-phenibut (23.3 μM) > baclofen (6.0 μM). Moreover, F-phenibut suppressed action potential generation in Purkinje cells. Reference: Eur J Pharmacol. 2020 Oct 5;884:173437. https://pubmed.ncbi.nlm.nih.gov/32735986/
In vivo activity:	The aim of the present study was to test the effects of R-phenibut on the motor, sensory and tactile functions and histological outcomes in rats following transient middle cerebral artery occlusion (MCAO). R-phenibut treatment at a dose of 50mg/kg significantly alleviated reduction of brain volume in damaged hemisphere in both f-MCAO and ET1-MCAO. In R-phenibut treated animals a trend of recovery of tactile and proprioceptive stimulation in the vibrissae-evoked forelimb-placing test was observed. After R-phenibut treatment at a dose of 50mg/kg statistically significant increase of BDNF and VEGF gene expression was found in damaged brain hemisphere. Reference: Pharmacol Res. 2016 Nov;113(Pt B):796-801. https://pubmed.ncbi.nlm.nih.gov/26621244/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	35.0	195.29

Preparing Stock Solutions

The following data is based on the product molecular weight 179.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Irie T, Yamazaki D, Kikura-Hanajiri R. F-phenibut (β-(4-Fluorophenyl)-GABA), a potent GABAB receptor agonist, activates an outward-rectifying K+ current and suppresses the generation of action potentials in mouse cerebellar Purkinje cells. Eur J Pharmacol. 2020 Oct 5;884:173437. doi: 10.1016/j.ejphar.2020.173437. Epub 2020 Jul 28. PMID: 32735986. 2. Belozertseva I, Nagel J, Valastro B, Franke L, Danysz W. Optical isomers of phenibut inhibit [H(3)]-Gabapentin binding in vitro and show activity in animal models of chronic pain. Pharmacol Rep. 2016 Jun;68(3):550-4. doi: 10.1016/j.pharep.2015.12.004. Epub 2015 Dec 22. PMID: 26894962. 3. Vavers E, Zvejniece L, Svalbe B, Volska K, Makarova E, Liepinsh E, Rizhanova K, Liepins V, Dambrova M. The neuroprotective effects of R-phenibut after focal cerebral ischemia. Pharmacol Res. 2016 Nov;113(Pt B):796-801. doi: 10.1016/j.phrs.2015.11.013. Epub 2015 Nov 24. PMID: 26621244. 4. Zvejniece L, Vavers E, Svalbe B, Veinberg G, Rizhanova K, Liepins V, Kalvinsh I, Dambrova M. R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects. Pharmacol Biochem Behav. 2015 Oct;137:23-9. doi: 10.1016/j.pbb.2015.07.014. Epub 2015 Jul 31. PMID: 26234470.
In vitro protocol:	1. Irie T, Yamazaki D, Kikura-Hanajiri R. F-phenibut (β-(4-Fluorophenyl)-GABA), a potent GABAB receptor agonist, activates an outward-rectifying K+ current and suppresses the generation of action potentials in mouse cerebellar Purkinje cells. Eur J Pharmacol. 2020 Oct 5;884:173437. doi: 10.1016/j.ejphar.2020.173437. Epub 2020 Jul 28. PMID: 32735986. 2. Belozertseva I, Nagel J, Valastro B, Franke L, Danysz W. Optical isomers of phenibut inhibit [H(3)]-Gabapentin binding in vitro and show activity in animal models of chronic pain. Pharmacol Rep. 2016 Jun;68(3):550-4. doi: 10.1016/j.pharep.2015.12.004. Epub 2015 Dec 22. PMID: 26894962.
In vivo protocol:	1. Vavers E, Zvejniece L, Svalbe B, Volska K, Makarova E, Liepinsh E, Rizhanova K, Liepins V, Dambrova M. The neuroprotective effects of R-phenibut after focal cerebral ischemia. Pharmacol Res. 2016 Nov;113(Pt B):796-801. doi: 10.1016/j.phrs.2015.11.013. Epub 2015 Nov 24. PMID: 26621244. 2. Zvejniece L, Vavers E, Svalbe B, Veinberg G, Rizhanova K, Liepins V, Kalvinsh I, Dambrova M. R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects. Pharmacol Biochem Behav. 2015 Oct;137:23-9. doi: 10.1016/j.pbb.2015.07.014. Epub 2015 Jul 31. PMID: 26234470.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

[1] Lapin I, et al. CNS Drug Rev. 2001, 7(4):471-81.

[2] Zyablitseva EA, et al. Neurosci Behav Physiol. 2008, 38(6):

Your view history

Phenibut featured