Baclofen

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

神经递质 GABA 的衍生物，充当 GABAB 受体激动剂。

A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist; also blocks α2δ subunit-containing voltage-dependent calcium channel (VDCC) with Ki of 156 uM; A neurotransmitter inhibitor by blocking the release of excitatory transmitters; serves as a central nervous system depressant and skeletal muscle relaxant.Other Indication Approved(In Vitro):Baclofen (1, 10 μM; 24 h) 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.(In Vivo):Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) ameliorates motor deficits in YAC128 HD transgenic mice.

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Animal Model:Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age 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.

Baclofen | Lioresal, Liofen, Gablofen | Baclon | Kemstro

Membrane Transporter/Ion Channel

GAT

GABAR

Other Indications

Other Disease

1134-47-0

213.6608

C10H12ClNO2

>98% (HPLC)

DMSO: < 7.8 mg/mL

O=C(O)CC(C1=CC=C(Cl)C=C1)CN

Benzenepropanoic acid, β-(aminomethyl)-4-chloro-

(-20℃)

With Ice Pack

≥ 2 years