(R)-baclofen (formerly STX-209; STX209; STX 209), a derivative of gamma-aminobutyric acid, is a selective GABAB receptor agonist that has been primarily used to treat spasticity. 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. GABAB receptors are metabotropic receptors which produce slow inhibitory signals.
理化性质和储存条件
| Molecular Weight (MW) | 213.66 |
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| Formula | C10H12ClNO2 |
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| CAS No. | 69308-37-8 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 8 mg/mL (37.4 mM) |
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| Water:<1 mg/mL |
| Ethanol:<1 mg/mL |
| SMILES | ClC1=CC=C([C@](CC(O)=O)([H])CN)C=C1 |
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| Synonyms | STX209; STX-209; STX 209; |
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实验参考方法
| In Vitro | In vitro activity: Baclofen is a skeletal muscle relaxant used in the treatment of spasticity of spinal and cerebral origin. Although it is marketed as a racemic mixture, only the baclofen R-enantiomer is stereospecifically active at so called GAGAB-receptors. Researchers believe that the enantiomers of baclofen have different properties. It is claimed that the R-(–)-enantiomer is about 100 times more active than the S-(+)-enantiomer. |
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| In Vivo | (R)-Baclofen (STX209) suppresses audiogenic seizures in the Fmr1-knockout mouse on the seizure-resistant C57BL/6 background with an effective dose of 1 mg/kg; Acute intraperitoneal administration of (R)-Baclofen (STX209) significantly reduces the percent of mice displaying seizures (seizure incidence), with a minimum effective dose (MED) of 1.5 mg/kg. |
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| Animal model | Mice |
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| Formulation & Dosage | 1, 1.5 mg/kg; i.p. |
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| References | J Neurochem. 1986 Sep;47(3):898-903; Lancet. 1984 May 12;1(8385):1078. |
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