Baclofen

For research use only.

Catalog No.S4840

Baclofen Chemical Structure

CAS No. 1134-47-0

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.

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Biological Activity

Description Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
Targets
GABAB receptor [2]
()
In vitro

Baclofen induces G0/G1 phase arrest which is connected with down-regulation of intracellular cAMP level, and up-regulation of p21WAF1 protein expression as well as its phosphorylation level in human hepatocellular carcinoma cell[3].

In vivo Chronic treatment with baclofen markedly diminishes hippocampal atrophy and neuronal apoptosis in hippocampal CA1 area via the regulation of autophagy in chronic cerebral hypoperfusion in rats. Baclofen might suppress cytodestructive autophagic activity through Akt-GSK-3β-p-mTOR-Beclin 1 signaling pathway under chronic cerebral hypoperfusion. During brain ischemia, baclofen could reduce CX43 and CX36 surface expression. Baclofen-induced suppression of increased CX43 and CX36 surface expressions helps neurons survive[1]. Baclofen reduces reinstatement to cocaine self-administration in an animal model of relapse[2]. Baclofen suppresses Bel-7402 xenograft tumor growth in vivo[3].

Protocol

Cell Research:[3]
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  • Cell lines: Bel-7402, HuH-7, and HepG2 cells
  • Concentrations: 25, 50 and 100 μM
  • Incubation Time: 0-4 days
  • Method: Bel-7402, HuH-7, and HepG2 cells are seeded into 96-well plates (10,000 per well) in a final volume of 200 μl medium. After a 24-hour attachment, cells are incubated with Bac (25, 50 and 100 μM) in the absence or presence of Pha (100 μM) for indicated time intervals. During this time, the culture medium is replaced with fresh medium every 24 h. After treatment, cell proliferation is evaluated by MTS assay. The OD values are measured at 490 nm with a microplate spectrophotometer.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: male Sprague-Dawley rats of clean grade, aged 2-3 months, weighing 220-250 g
  • Dosages: 12.5 mg/kg and 25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro 3 mg/mL warmed (14.04 mM)
Water 0.1 mg/mL (0.46 mM)
DMSO Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 213.66
Formula

C10H12ClNO2

CAS No. 1134-47-0
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=CC=C1C(CC(=O)O)CN)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04603625 Recruiting Other: postural management Quadriplegic Cerebral Palsy Azienda Unità Sanitaria Locale Reggio Emilia|Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta|Ospedale IRCCS G. Gaslini di Genova|IRCCS Eugenio Medea|IRCCS Don Carlo Gnocchi di Firenze|Azienda Unita'' Sanitaria Locale Di Modena|Azienda Usl di Bologna|Azienda Unità Sanitaria Locale Romagna|Azienda ULSS di Verona e Provincia|Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico September 1 2020 Not Applicable
NCT04509336 Active not recruiting Drug: Orphenadrine|Drug: Baclofen Cirrhosis Mansoura University August 20 2020 Not Applicable
NCT04471714 Recruiting Drug: Baclofen Spasticity Muscle|Spinal Cord Injuries University of Alberta January 10 2020 Phase 2
NCT03682978 Recruiting Drug: Arbaclofen|Drug: Placebo Autism Spectrum Disorder Celso Arango MD PhD|UMC Utrecht September 19 2019 Phase 2
NCT02760992 Unknown status Drug: IV Baclofen|Drug: Oral Baclofen Intravenous Baclofen Allaysis LLC|University of Minnesota May 2017 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID