巴氯芬盐酸盐

• 常用名: 巴氯芬盐酸盐
• 英文名: Baclofen hydrochloride
• CAS号: 28311-31-1
• 分子量: 250.12
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₀H₁₃Cl₂NO₂
• 熔点: N/A
• 闪点: N/A

巴氯芬盐酸盐用途

盐酸巴氯芬是γ-氨基丁酸(GABA)的亲脂性衍生物,是一种口服活性、选择性代谢性GABAB受体(GABABR)激动剂。盐酸巴氯芬模拟GABA的作用,通过GABAB受体产生缓慢的突触前抑制。盐酸巴氯芬具有高血脑屏障外显率。盐酸巴氯芬具有肌肉痉挛研究的潜力[1][2][3]。

巴氯芬盐酸盐名称

• 中文名: 巴氯芬盐酸盐
• 英文名: Baclofen hydrochloride

巴氯芬盐酸盐生物活性

• 描述: 盐酸巴氯芬是γ-氨基丁酸(GABA)的亲脂性衍生物,是一种口服活性、选择性代谢性GABAB受体(GABABR)激动剂。盐酸巴氯芬模拟GABA的作用,通过GABAB受体产生缓慢的突触前抑制。盐酸巴氯芬具有高血脑屏障外显率。盐酸巴氯芬具有肌肉痉挛研究的潜力[1][2][3]。
• 相关类别:
  信号通路 >> 跨膜转运 >> GABA受体
  研究领域 >> 神经疾病
  信号通路 >> 神经信号通路 >> GABA受体
• 体外研究: 盐酸巴氯芬(1,10μM；24小时)导致乳酸脱氢酶(LDH)活性显著降低,表明野生型或突变型亨廷顿蛋白表达纹状体细胞(HD19或HD43)的细胞活力增加。巴氯芬显著增加了HD43细胞中的糜蛋白酶样蛋白酶体活性和细胞活力[3]。
• 体内研究: 盐酸巴氯芬(口服；10μg/g；每日两次,连续3天)可改善YAC128 HD转基因小鼠的运动障碍[3]。动物模型：13-18个月龄的野生型(WT)和突变型(MT)雄性YAC128小鼠[3]剂量：10μg/g给药：IP；每天两次,上午9:00和下午5:00,连续3天；然后在第四天上午9:00单次给药结果：改善YAC128 HD转基因小鼠的运动障碍。在YAC128 HD转基因小鼠中增加蛋白酶体活性并减少神经元核内内含物(NII)。
• 参考文献:

  [1]. 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.

  [2]. Bexis, S., et al., Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend, 2004. 74(1): p. 89-96.

  [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.

巴氯芬盐酸盐物理化学性质

• 分子式: C₁₀H₁₃Cl₂NO₂
• 分子量: 250.12
• InChIKey: WMNUVYYLMCMHLU-UHFFFAOYSA-N
• SMILES: Cl.NCC(CC(=O)O)c1ccc(Cl)cc1

巴氯芬盐酸盐靶点实验

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