Baclofen hydrochloride

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CAS NO:

28311-31-1

巴氯芬盐酸盐

Baclofen hydrochloride 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物，是一种口服有效，选择性的代谢型 GABA_B受体 (GABA_BR) 激动剂。Baclofen hydrochloride 可以模拟 GABA 的作用并通过 GABA_B受体产生缓慢的突触前抑制。Baclofen hydrochloride 具有高的血脑屏障透过率。Baclofen hydrochloride 有用于肌肉痉挛研究的潜力。

生物活性

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

体外研究
(In Vitro)

Baclofen (1, 10 μM; 24 h) hydrochloride causes markedly decreased lactate dehydrogenase (LDH) activity, indicating increased cell viability in wild-type or mutant huntingtin-expressing striatal cells (HD19 or HD43). Baclofen significantly increases chymotrypsin-like proteasome activity and cell viability were in the HD43 cells^[3].

体内研究
(In Vivo)

Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) hydrochloride ameliorates motor deficits in YAC128 HD transgenic mice^[3].

Animal Model:	Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age^[3]
Dosage:	10 μg/g
Administration:	IP; twice daily at 9:00 a.m. and 5:00 p.m., for 3 consecutive days; then single dose on the fourth day at 9:00 a.m
Result:	Ameliorated motor deficits in YAC128 HD transgenic mice. Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.

Clinical Trial

分子量

250.12

Formula

C₁₀H₁₃Cl₂NO₂

CAS 号

28311-31-1

中文名称

巴氯芬盐酸盐；盐酸巴氯芬

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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