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(R)-Baclofen(STX209)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(R)-Baclofen(STX209)图片
CAS NO:69308-37-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
(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
FormulaC10H12ClNO2
CAS No.69308-37-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 8 mg/mL (37.4 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
SMILESClC1=CC=C([C@](CC(O)=O)([H])CN)C=C1
SynonymsSTX209; STX-209; STX 209;
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.

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.
Animal modelMice
Formulation & Dosage1, 1.5 mg/kg; i.p.
References

J Neurochem. 1986 Sep;47(3):898-903; Lancet. 1984 May 12;1(8385):1078.