Metaxalone-d₃  (Synonyms: 美他沙酮 d₃)

Metaxalone-d₃ is the deuterium labeled 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][3][4].

PPARγ and MAO-A^[4]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

224.27

C₁₂H₁₂D₃NO₃

1192812-66-0

1665-48-1

固体

White to off-white

美他沙酮 d₃

Room temperature in continental US; may vary elsewhere.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. http://en.wikipedia.org/wiki/Metaxalone

  [3]. Stanko JR. Review of oral skeletal muscle relaxants for the craniomandibular disorder (CMD) practitioner. Cranio. 1990 Jul;8(3):234-43.  [Content Brief]

  [4]. Pallio G, et al. MAO-A Inhibition by Metaxalone Reverts IL-1β-Induced Inflammatory Phenotype in Microglial Cells. Int J Mol Sci. 2021;22(16):8425.  [Content Brief]