WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317307
CAS#: 1134-47-0
Description: 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.
Hodoodo Cat#: H317307
Name: Baclofen
CAS#: 1134-47-0
Chemical Formula: C10H12ClNO2
Exact Mass: 213.06
Molecular Weight: 213.660
Elemental Analysis: C, 56.21; H, 5.66; Cl, 16.59; N, 6.56; O, 14.98
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:
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| Water | 2.0 | 9.50 | |
| 0.01M HCl | 3.0 | 14.04 |
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: | 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. |
| 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.
