Baclofen-d₅ hydrochloride  (Synonyms: 巴氯芬盐酸盐-d₅)

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research^[1][2][3].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Baclofen (1，10 μM；24 h) 导致乳酸脱氢酶 (LDH) 活性显著降低，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。Baclofen 显著增加 HD43 细胞中的胰凝乳蛋白酶样蛋白酶体活性和细胞活力^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Baclofen (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^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

255.15

C₁₀H₈D₅Cl₂NO₂

2012598-58-0

1134-47-0

巴氯芬盐酸盐-d₅；氯苯氨丁酸盐酸盐-d₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

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