(R)-巴氯芬 (Arbaclofen) 是一种选择性 GABAB 受体激动剂。
| Cas No. | 69308-37-8 |
| 别名 | (R)-巴氯芬; Arbaclofen; STX209 |
| 化学名 | (3R)-4-amino-3-(4-chlorophenyl)butanoic acid |
| Canonical SMILES | C1=CC(=CC=C1C(CC(=O)O)CN)Cl |
| 分子式 | C10H12ClNO2 |
| 分子量 | 213.66 |
| 溶解度 | ≥ 7.13mg/mL in H20 with gentle warming |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | (R)-Baclofen(STX209) is a selective GABAB receptor agonist[1]. (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 [5].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[5]. References:
[1]. Falch E, Hedegaard A, Nielsen L 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.
[2]. Henderson C, et al. Reversal of disease-related pathologies in the fragile X mouse model by selective activation of GABAB receptors with arbaclofen. Sci Transl Med. 2012 Sep 19;4(152):152ra128.
[3]. Hong YG, Henry JL. 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.
[4]. Orsnes G, Crone C, Krarup C 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.
[5]. Colombo G, Addolorato G, Agabio R et al. Role of GABA(B) receptor in alcohol dependence: reducing effect of baclofen on alcohol intake and alcohol motivational properties in rats and amelioration of alcohol withdrawal syndrome and alcohol craving in human alcoholics. Neurotox Res. 2004;6(5):403-14.
[6]. Stetkarova I, Yablon SA, Kofler M, Stokic DS. Procedure- and device-related complications of intrathecal baclofen administration for management of adult muscle hypertonia: a review. Neurorehabil Neural Repair. 2010 Sep;24(7):609-19. |
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