Metaxalone

Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia^[1][2]. IC50 & Target:PPARγ and MAO-A^[1] In Vitro:Metaxalone (10-40 µg/mL; 1 h) reverses the inflammatory phenotype of IL-1β-treated HMC3 cells, decreases the expression of pro-inflammatory factors TNF-α and IL-6, and increases the expression of anti-inflammatory factor IL-13^[1].
Metaxalone (10-40 µg/mL; 1 h) shows antioxidant properties in IL-1β-treated HMC3 cells, significantly upregating Nrf2 levels and decreasing MDA levels^[1].
Metaxalone (10-40 µg/mL; 1 h) inhibits the increase of NF-κB and stimulates the activation of PPARγ and PGC-1α in IL-1β-treated HMC3 cells^[1].
Metaxalone (10-40 µg/mL; 1 h) inhibits MAO-A activity in a dose-dependent manner^[1].
Metaxalone (10-40 µg/mL; 24-72 h) has no cytotoxic effect on HMC3 cells^[1].