Chemical Name:2-Amino-N-(1-methyl-1,2-diphenylethyl)acetamide
hydrochloride
Biological Activity:
Uncompetitive
NMDA receptor antagonist; blocks ion channel and allosteric modulatory site (IC50
= 8-68 μM). Anticonvulsant in vivo and metabolises to a more potent
desglycine analogue. Weakly blocks voltage-dependent Na+ channels
(IC50 = 161 μM).
Palmeret al (1995) Neuroprotective
properties of the uncompetitive NMDA receptor antagonist remacemide
hydrochloride. Ann.N.Y.Acad.Sci. 765 236. Subramaniamet
al (1996) Block of the N-methyl-D-aspartate
receptor by remacemide and its des-glycine metabolite.
J.Pharmacol.Exp.Ther. 276 161. Santangeli et al (2002)
Na(+) channel effects of remacemide and desglycinyl-remacemide in rat cortical
synaptosomes. Eur.J.Pharmacol. 438 63.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.