(±)-Baclofen
Catalog No.: GC12927Purity:>98.00%
(±)-Baclofen is a lipophilic derivative of γ-aminobutyric acid (GABA), and it is an orally effective and selective agonist of the metabotropic GABAB receptor with an IC50 of 200nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1134-47-0
5gIn Stock
$74.00
1
10gIn Stock
$133.00
1
25gIn Stock
$244.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 5g | $74.00 | In Stock | 1 | |
| 10g | $133.00 | In Stock | 1 | |
| 25g | $244.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
1 publicationsPublications from researchers using this productDescription
(±)-Baclofen is a lipophilic derivative of γ-aminobutyric acid (GABA), and it is an orally effective and selective agonist of the metabotropic GABAB receptor with an IC50 of 200nM [1-2]. GABA is an inhibitory neurotransmitter that functions through heteromeric ligand-gated ion channels GABAA and GABAC as well as G protein-coupled receptors GABAB [3]. (±)-Baclofen can be used as a relaxant for muscle spasms and a central nervous system inhibitor [4].
In vitro, (±)-Baclofen (25, 50, and 100μM; 24, 48, 72, and 96h) inhibited the proliferation of HepG2 cells in a dose-dependent manner, downregulated intracellular cAMP levels, and upregulated the expression and phosphorylation of p21WAF1 protein. (±)-Baclofen also caused cell cycle arrest in the G0/G1 phase without inducing cell death [3]. (±)-Baclofen (1, 10μM; 24h) significantly reduced the activity of lactate dehydrogenase (LDH) in high-density model (HD) striatal cells (HD19 and HD43), enhanced the activity of cathepsin-like proteasome in the cells and cell viability [5].
In vivo, 30 minutes before behavioral tests, intraperitoneal injection of (±)-Baclofen (0.5, 1.5, and 2.5mg/kg/d; single-dose) enhanced the alcohol consumption behavior of mice in the Vogel conflict test, which might be due to the analgesic effect of Baclofen. Mice treated with (±)-Baclofen showed similar sedative effects in other tests (i.e., reduced activity) [6]. (±)-Baclofen (4mg/kg/d; 4d; i.p.) reversed the increase in the frequency of voluntary mouth-chewing movements (VCM) induced by reserpine in mice. After repeated treatment, (±)-Baclofen reduced the spontaneous systemic activity in mice induced by reserpine. [7].
References:
[1] Lin F, Cao Z, Hosford D A. Increased number of GABAB receptors in the lethargic (lh/lh) mouse model of absence epilepsy[J]. Brain research, 1993, 608(1): 101-106.
[2] Farokhnia M, Deschaine SL, Sadighi A, et al. A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: lessons learned from a human laboratory investigation. Mol Psychiatry. 2021;26(2):545-555.
[3] Wang T, Huang W, Chen F. Baclofen, a GABAB receptor agonist, inhibits human hepatocellular carcinoma cell growth in vitro and in vivo. Life Sci. 2008;82(9-10):536-541.
[4] DeFalco A P. Neuromuscular blocking agents and skeletal muscle relaxants[M]//Side Effects of Drugs Annual. Elsevier, 2024, 46: 171-180.
[5] Kim W, Seo H. Baclofen, a GABAB receptor agonist, enhances ubiquitin-proteasome system functioning and neuronal survival in Huntington's disease model mice. Biochem Biophys Res Commun. 2014;443(2):706-711.
[6] Li X, Risbrough VB, Cates-Gatto C, et al. Comparison of the effects of the GABAB receptor positive modulator BHF177 and the GABAB receptor agonist baclofen on anxiety-like behavior, learning, and memory in mice. Neuropharmacology. 2013; 70:156-167.
[7] Castro JP, Frussa-Filho R, Fukushiro DF, et al. Effects of baclofen on reserpine-induced vacuous chewing movements in mice. Brain Res Bull. 2006;68(6):436-441.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
HepG2 cells |
|
Preparation Method |
HepG2 cells were seeded into 96-well plates (10,000 per well) in a final volume of 200μl medium. After a 24-hour attachment, cells were incubated with (±)-Baclofen (25, 50 and 100μM) in the absence or presence of Pha (100μM) for indicated time intervals. During this time, the culture medium was replaced with fresh medium every 24h. After treatment, cell proliferation was evaluated by 3-(4, 5-dimethylthiazol-2-yl)5-(3-carboxymethoxyphenyl)2-(4-sulfophenyl)2H-tetrazolium, inner salt (MTS) assay. The OD values were measured at 490nm with a microplate spectrophotometer (Molecular Devices). |
|
Reaction Conditions |
25, 50 and 100μM; 24, 48, 72, and 96h |
|
Applications |
(±)-Baclofen inhibited the proliferation of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6J mice |
|
Preparation Method |
(±)-Baclofen was dissolved in sterile 0.9% saline and injected intraperitoneally (i.p.) 30min before testing. BHF177 was suspended in 0.5% methylcellulose and administered orally (p.o.) 60min before testing. The convulsant drug PTZ was dissolved in sterile 0.9% saline and injected i.p. immediately before testing. The doses of (±)-Baclofen (0.5, 1.5, and 2.5mg/kg) and route of administration (i.p.) were chosen based on previously published studies that all reported a narrow effective dose range of this compound before sedative effects were manifested. The doses of BHF177 (10, 20, and 40mg/kg) and route of administration (p.o.) were also chosen based on previous studies. All of the drugs were administered in volumes of 0.1ml/10g body weight in mice. The effects of (±)-baclofen and BHF177 were studied by using the "between-group design". Behavioral tests were designed, and the sample size for each group was 12. |
|
Dosage form |
0.5, 1.5, and 2.5mg/kg/d; Single-dose; i.p. |
|
Applications |
(±)-Baclofen treatment increased the alcohol consumption behavior of mice in the Vogel conflict test. This phenomenon might be due to the analgesic effect of (±)-Baclofen. Mice treated with (±)-Baclofen also showed similar sedative effects in other tests (i.e., reduced activity). |
|
References: |
|
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
1134-47-0
Chemical Name
β-(aminomethyl)-4-chloro-benzenepropanoic acid
SMILES
ClC1=CC=C(C(CN)CC(O)=O)C=C1
Molecular Formula
C10H12ClNO2
Molecular Weight
213.7
Solubility
0.1 M HCl : 10 mg/mL (46.80 mM; Need ultrasonic); DMSO : 4.81 mg/mL (22.51 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 60°C); H2O : 2 mg/mL (9.36 mM; Need ultrasonic)
Storage
Store at 2-8°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
Review for (±)-Baclofen
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%