(R)-Baclofen | (R)-巴氯芬

MCE 国际站：(R)-Baclofen

中文名：(R)-巴氯芬

CAS：69308-37-8

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：(R)-Baclofen (Arbaclofen) 是一种选择性 GABAB 受体激动剂^[1]。 IC50 和靶标：GABAB 受体^[1] 

体内：(R)-Baclofen (STX209) 以 1 mg/kg 的有效剂量抑制 Fmr1-knockout 小鼠在抗癫痫发作的 C57BL/6 背景下的听源性癫痫发作 ^{[5].(R)-巴氯芬 (STX209) 的急性腹膜内给药显着降低了小鼠出现癫痫发作的百分比（癫痫发作发生率），最小有效剂量 (MED) 为 1.5 mg/kg[5 ]。}

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研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

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参考文献：[1]. Hong YG, et al. Effects of phaclofen and the enantiomers of baclofen on cardiovascular responses to intrathecal administration of L- and D-baclofen in the rat. Eur J Pharmacol. 1991 Apr 24;196(3):267-75.

[2]. Falch E, et al. Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations. J Neurochem. 1986 Sep;47(3):898-903.

[3]. Orsnes G, et al. The effect of baclofen on the transmission in spinal pathways in spastic multiple sclerosis patients. Clin Neurophysiol. 2000 Aug;111(8):1372-9.