Baclofen | CAS#1134-47-0 | GABA-B Antagonist

MedKoo Cat#: 317307 | Name: Baclofen

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Description:

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

Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Chemical Structure

Baclofen

CAS#1134-47-0

Theoretical Analysis

MedKoo Cat#: 317307

Name: Baclofen

CAS#: 1134-47-0

Chemical Formula: C10H12ClNO2

Exact Mass: 213.0557

Molecular Weight: 213.66

Elemental Analysis: C, 56.21; H, 5.66; Cl, 16.59; N, 6.56; O, 14.98

Price and Availability

Size	Price	Availability	Quantity
1g	USD 250.00	2 Weeks
5g	USD 450.00	2 Weeks

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Related CAS #

1134-47-0 63701-56-4 (S-isomer HCl) 66514-99-6 (S-isomer free base)

Synonym

Baclofen; Lioresal, Liofen, Gablofen; Baclon; Kemstro

IUPAC/Chemical Name

4-amino-3-(4-chlorophenyl)butanoic acid

InChi Key

KPYSYYIEGFHWSV-UHFFFAOYSA-N

InChi Code

InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)

SMILES Code

O=C(O)CC(C1=CC=C(Cl)C=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, not in water

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:

Baclofen is a GABA-B receptor (GABABR) agonist.

In vitro activity:

Baclofen (bath applied at 10 microM) caused a 10-15 mV hyperpolarization of CA3 cells and a 75-100% decrease in the amplitude of excitatory and inhibitory postsynaptic potentials (EPSPs and IPSPs). Baclofen reduced the amplitude of monosynaptic IPSPs elicited in the presence of excitatory amino acid receptor antagonists, as well as the amplitude of EPSPs elicited after blocking GABAA receptors and reducing subsequent epileptic bursts with excitatory amino acid receptor antagonists. Reference: J Physiol. 1992;451:329-45. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1176164/

In vivo activity:

The effects of the in vivo administration of baclofen on renal tubular transport and aquaporin-2 (AQP2) expression were evaluated. In conscious rats kept in metabolic cages, baclofen (0.01-1mg/kg, s.c.) induced a dose-dependent increment in the urine flow rate (UFR) and in sodium and potassium excretion, associated with an increased osmolal clearance (Closm), a diminished urine to plasma osmolality ratio (Uosm/Posm) and a decrease in AQP2 expression. Reference: Eur J Pharmacol. 2013 Sep 5;715(1-3):117-22. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1176164/

	Solvent	mg/mL	mM
Solubility
	Water	2.0	9.50
	0.01M HCl	3.0	14.04

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 213.66 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. Thompson SM, Gähwiler BH. Comparison of the actions of baclofen at pre- and postsynaptic receptors in the rat hippocampus in vitro. J Physiol. 1992;451:329-45. doi: 10.1113/jphysiol.1992.sp019167. PMID: 1328619; PMCID: PMC1176164. 2. Donato V, Pisani GB, Trumper L, Monasterolo LA. Effects of "in vivo" administration of baclofen on rat renal tubular function. Eur J Pharmacol. 2013 Sep 5;715(1-3):117-22. doi: 10.1016/j.ejphar.2013.05.042. Epub 2013 Jun 18. PMID: 23791849.

In vitro protocol:

In vivo protocol:

1. Donato V, Pisani GB, Trumper L, Monasterolo LA. Effects of "in vivo" administration of baclofen on rat renal tubular function. Eur J Pharmacol. 2013 Sep 5;715(1-3):117-22. doi: 10.1016/j.ejphar.2013.05.042. Epub 2013 Jun 18. PMID: 23791849.

1: Hasnat MJ, Rice JE. Intrathecal baclofen for treating spasticity in children with cerebral palsy. Cochrane Database Syst Rev. 2015 Nov 13;11:CD004552. [Epub ahead of print] Review. PubMed PMID: 26563961. 2: Ingale H, Ughratdar I, Muquit S, Moussa AA, Vloeberghs MH. Selective dorsal rhizotomy as an alternative to intrathecal baclofen pump replacement in GMFCS grades 4 and 5 children. Childs Nerv Syst. 2015 Nov 9. [Epub ahead of print] PubMed PMID: 26552383. 3: Hajj R, Milet A, Toulorge D, Cholet N, Laffaire J, Foucquier J, Robelet S, Mitry R, Guedj M, Nabirotchkin S, Chumakov I, Cohen D. Combination of acamprosate and baclofen as a promising therapeutic approach for Parkinson's disease. Sci Rep. 2015 Nov 6;5:16084. doi: 10.1038/srep16084. PubMed PMID: 26542636. 4: Scarpellini E, Boecxstaens V, Broers C, Vos R, Pauwels A, Tack J. Effect of baclofen on gastric acid pocket in subjects with gastroesophageal reflux disease symptoms. Dis Esophagus. 2015 Nov 6. doi: 10.1111/dote.12443. [Epub ahead of print] PubMed PMID: 26541138. 5: Nahar LK, Cordero RE, Nutt D, Lingford-Hughes A, Turton S, Durant C, Wilson S, Paterson S. Validated Method for the Quantification of Baclofen in Human Plasma Using Solid-Phase Extraction and Liquid Chromatography-Tandem Mass Spectrometry. J Anal Toxicol. 2015 Nov 4. pii: bkv125. [Epub ahead of print] PubMed PMID: 26538544. 6: Zheng K, Brodsky JB. Spinal Surgery and Abrupt Intrathecal Baclofen Withdrawal. A A Case Rep. 2015 Nov 1;5(9):160-1. doi: 10.1213/XAA.0000000000000215. PubMed PMID: 26528702. 7: Clearfield JS, Nelson ME, McGuire J, Rein LE, Tarima S. Intrathecal Baclofen Dosing Regimens: A Retrospective Chart Review. Neuromodulation. 2015 Oct 30. doi: 10.1111/ner.12361. [Epub ahead of print] PubMed PMID: 26517855. 8: Sayer C, Lumsden DE, Perides S, Tustin K, Bassi S, Lin JP, Kaminska M. Intrathecal baclofen trials: complications and positive yield in a pediatric cohort. J Neurosurg Pediatr. 2015 Oct 30:1-6. [Epub ahead of print] PubMed PMID: 26517061. 9: Shibata A, Yamamoto M, Watanabe Y, Terashima H, Kashii H, Kubota M, Morota N. [Scintigraphic imaging in the diagnosis of failed intrathecal baclofen therapy: a case report of a 7-year-old boy with ventriculoperitoneal shunt]. No To Hattatsu. 2015 Sep;47(5):367-71. Japanese. PubMed PMID: 26502655. 10: McCormick ZL, Chu SK, Binler D, Neudorf D, Mathur SN, Lee J, Marciniak C. Intrathecal versus Oral Baclofen; a Matched Cohort Study of Spasticity, Pain, Sleep, Fatigue and Quality of Life. PM R. 2015 Oct 20. pii: S1934-1482(15)01065-5. doi: 10.1016/j.pmrj.2015.10.005. [Epub ahead of print] PubMed PMID: 26498518. 11: Medical Cost Impact of Intrathecal Baclofen Therapy for Severe Spasticity. Neuromodulation. 2015 Oct;18(7):650. doi: 10.1111/ner.12355. PubMed PMID: 26477603. 12: Brown JW, Moeller A, Schmidt M, Turner SC, Nimmrich V, Ma J, Rueter LE, van der Kam E, Zhang M. Anticonvulsant effects of structurally diverse GABA(B) positive allosteric modulators in the DBA/2J audiogenic seizure test: Comparison to baclofen and utility as a pharmacodynamic screening model. Neuropharmacology. 2015 Oct 20;101:358-369. doi: 10.1016/j.neuropharm.2015.10.009. [Epub ahead of print] PubMed PMID: 26471422. 13: Weibel S, Lalanne L, Riegert M, Bertschy G. Efficacy of High-Dose Baclofen for Alcohol Use Disorder and Comorbid Bulimia: A Case Report. J Dual Diagn. 2015 Oct 12:0. [Epub ahead of print] PubMed PMID: 26457456. 14: Salte K, Lea G, Franek M, Vaculin S. Baclofen reversed thermal place preference in rats with chronic constriction injury. Physiol Res. 2015 Oct 8. [Epub ahead of print] PubMed PMID: 26447518. 15: Chaignot C, Weill A, Ricordeau P, Alla F. [Use in France of Baclofen for Alcohol Dependence from 2007 to 2013: Cohort Study Based on the Databases SNIIRAM and PMSI]. Therapie. 2015 Sep-Oct;70(5):443-53. doi: 10.2515/therapie/2015027. Epub 2015 Jun 26. French. PubMed PMID: 26423143. 16: Baclofen and pregnancy: birth defects and withdrawal symptoms. Prescrire Int. 2015 Sep;24(163):214. PubMed PMID: 26417633. 17: Cleophax C, Goncalves A, Chasport C, de Beaugrenier E, Labat L, Declèves X, Mégarbane B. Usefulness of plasma drug monitoring in severe baclofen poisoning. Clin Toxicol (Phila). 2015 Nov;53(9):1-2. doi: 10.3109/15563650.2015.1088158. PubMed PMID: 26415080. 18: Liu L, Li CJ, Lu Y, Zong XG, Luo C, Sun J, Guo LJ. Baclofen mediates neuroprotection on hippocampal CA1 pyramidal cells through the regulation of autophagy under chronic cerebral hypoperfusion. Sci Rep. 2015 Sep 28;5:14474. doi: 10.1038/srep14474. PubMed PMID: 26412641; PubMed Central PMCID: PMC4585985. 19: Sechrist C, Kinsman S, Cain N. Profound Bradycardia After Intrathecal Baclofen Injection in a Patient With Hydranencephaly. Pediatr Neurol. 2015 Aug 28. pii: S0887-8994(15)00419-1. doi: 10.1016/j.pediatrneurol.2015.08.010. [Epub ahead of print] PubMed PMID: 26411756. 20: Reichmuth P, Blanc AL, Tagan D. Unintentional baclofen intoxication in the management of alcohol use disorder. BMJ Case Rep. 2015 Sep 22;2015. pii: bcr2015212187. doi: 10.1136/bcr-2015-212187. PubMed PMID: 26396128.