Memantine-d₆ hydrochloride  (Synonyms: 盐酸美金刚 d₆ (盐酸盐))

Memantine-d₆ (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].

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.

221.80

C₁₂H₁₆D₆ClN

1189713-18-5

41100-52-1

固体

White to off-white

盐酸美金刚 d₆ (盐酸盐)

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]. Robinson, D.M. and G.M. Keating, Memantine: a review of its use in Alzheimer's disease. Drugs, 2006. 66(11): p. 1515-34.  [Content Brief]

  [3]. Chen, H.S., et al., Open-channel block of N-methyl-D-aspartate (NMDA) responses by memantine: therapeutic advantage against NMDA receptor-mediated neurotoxicity. J Neurosci, 1992. 12(11): p. 4427-36.  [Content Brief]

  [4]. Chen, H.S. and S.A. Lipton, Mechanism of memantine block of NMDA-activated channels in rat retinal ganglion cells: uncompetitive antagonism. J Physiol, 1997. 499 ( Pt 1): p. 27-46.  [Content Brief]