Home Neuronal Signaling GABA Receptor agonist Baclofen For research use only.

Baclofen

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.

Baclofen Chemical Structure

Baclofen Chemical Structure

CAS No. 1134-47-0

Purity & Quality Control

Batch: S484001 0.01M HCl]3 mg/mL]true]Water]0.1 mg/mL]false]DMSO]Insoluble]false Purity: 99.79%
99.79

Baclofen Related Products

Signaling Pathway

GABA Receptor Signaling Pathways

GABA Receptor Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06175507 Not yet recruiting
Alcohol Liver Disease
Institute of Liver and Biliary Sciences India
 December 25 2023 Not Applicable
NCT04603625 Active not recruiting
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 della Romagna|Azienda ULSS di Verona e Provincia|Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico
 October 29 2020 Not Applicable
NCT04509336 Terminated
Cirrhosis
Mansoura University
 August 20 2020 Not Applicable
NCT04471714 Withdrawn
Spasticity Muscle|Spinal Cord Injuries
University of Alberta
 January 10 2020 Phase 2
NCT03682978 Completed
Autism Spectrum Disorder
Celso Arango MD PhD|UMC Utrecht
 September 19 2019 Phase 2

Chemical Information & Solubility

Molecular Weight 213.66 Formula

C10H12ClNO2
CAS No. 1134-47-0 SDF --
Smiles C1=CC(=CC=C1C(CC(=O)O)CN)Cl
Storage (From the date of receipt)

In vitro
Batch:

0.01M HCl : 3 mg/mL

Water : 0.1 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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