Memantine HCl | NMDA antagonist / Anti-Alzheimer’s

Memantine HCl (CAS 41100-52-1) is an NMDA noncompetitive, low affinity, open channel blocker, IC₅₀~1 mM at   -60 mV in rat retinal ganglion cells.¹ Displays neuroprotective effects in excitotoxic conditions.² Preferentially blocks excessive NMDA receptor activity without disrupting normal activity.³ A clinically well tolerated drug with therapeutic potential in numerous CNS degenerative disorders.⁴ In clinical use for Alzheimer’s disease.⁵

References/Citations:

1) Chen and Lipton (1997), Mechanism of memantine block of NMDA-activated channels in rat retinal ganglion cells: uncompetitive antagonism; J. Physiol. 499 27
2) Chen et al. (1998), Neuroprotective concentrations of the N-methyl-D-aspartate open-channel blocker memantine are effective without cytoplasmic vacuolation following post-ischemic administration and do not block maze learning or long-term potentiation; Neuroscience 86 1121
3) Lipton et al. (2005), The molecular basis of memantine action in Alzheimer’s disease and other neurologic disorders: low-affinity, uncompetitive antagonism; Curr. Alzheimer. Res. 2 155
4) Parsons et al. (1999), Memantine is a clinically well tolerated N-methyl-D-aspartate (NMDA) receptor antagonist—a review of preclinical data; Neuropharmacology 38 735
5) Witt et al. (2004), Memantine hydrochloride; Nat. Rev. Drug Discov. 3 109