Baclofen

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.