(±)-Baclofen |
Catalog No.GC12927
One-Click Copy Product Info
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(±)-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
Sample solution is provided at 25 µL, 10mM.
(±)-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.
| Cell experiment [1]: | |
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Cell lines |
HepG2 cells |
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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). |
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Reaction Conditions |
25, 50 and 100μM; 24, 48, 72, and 96h |
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Applications |
(±)-Baclofen inhibited the proliferation of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice |
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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. |
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Dosage form |
0.5, 1.5, and 2.5mg/kg/d; Single-dose; i.p. |
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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). |
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References: |
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| Cas No. | 1134-47-0 | SDF | |
| Chemical Name | β-(aminomethyl)-4-chloro-benzenepropanoic acid | ||
| Canonical SMILES | ClC1=CC=C(C(CN)CC(O)=O)C=C1 | ||
| Formula | C10H12ClNO2 | M.Wt | 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6795 mL | 23.3973 mL | 46.7946 mL |
| 5 mM | 935.9 μL | 4.6795 mL | 9.3589 mL |
| 10 mM | 467.9 μL | 2.3397 mL | 4.6795 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)