Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA B receptor (GABA B R) 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.
性状
Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) ameliorates motor deficits in YAC128 HD transgenic mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: H2O : 2 mg/mL (9.36 mM; Need ultrasonic)DMSO : < 1 mg/mL (insoluble or slightly soluble)配制储备液