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MCE 国际站:Baclofen
中文名:巴氯芬
CAS:1134-47-0
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:巴氯芬是 γ-氨基丁酸 (GABA) 的亲脂性衍生物,是一种具有口服活性的选择性代谢型 GABAB 受体 (GABABR)激动剂。 Baclofen 模仿 GABA 的作用,通过 GABAB 受体产生缓慢的突触前抑制。巴氯芬具有高血脑屏障渗透率。巴氯芬具有肌肉痉挛研究的潜力[1][2][3]。
体外:Baclofen (1, 10 μM; 24 h) 导致乳酸脱氢酶 (LDH) 活性显着降低,表明表达野生型或突变亨廷顿蛋白的纹状体细胞(HD19 或 HD43)的细胞活力增加。巴氯芬显着增加 HD43 细胞中的胰凝乳蛋白酶样蛋白酶体活性和细胞活力[3]。
体内:巴氯芬(ip;10 μg/g;每天两次,连续 3 天)改善 YAC128 HD 转基因小鼠的运动缺陷[3]。
热销产品:GN44028 | N-Methylnicotinamide | Rivastigmine | 4-Hydroxyphenylpyruvic acid | Parecoxib (Sodium) | LE135 | PF 1022A | 3-Oxocholic acid | Sulfapyridine | Crocetin
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:GABA Receptor
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Bexis, S., et al., Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend, 2004. 74(1): p. 89-96.
[2]. Mehdi Farokhnia, 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. 2018 Oct 31.
[3]. Woori Kim, et al. Baclofen, a GABAB receptor agonist, enhances ubiquitin-proteasome system functioning and neuronal survival in Huntington's disease model mice. Biochem Biophys Res Commun. 2014 Jan 10;443(2):706-11.
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