3，5-dimethyl-Tricyclo[3.3.1.13,7]decan-1-amine

Description

Memantine, a NMDA receptor antagonist, was co-developed by Forest Laboratories with Merz Pharmaceuticals and marketed under the trade name Namenda for the treatment of Alzheimer’s disease in the US after its approval in October, 2003. This drug has been available in many European and Asian markets before getting approval in the US.

Chemical Properties

White crystalline powder

in vitro

Memantine（3，5-dimethyl-Tricyclo[3.3.1.13,7]decan-1-amine） is an NMDA receptor antagonist that blocks NMDA-induced currents in rat retinal ganglion cells by 90% when used at a concentration of 12 μM. It reverses inhibition of dephosphorylation of the synthetic tau phosphopeptide p17 (tau194-207) induced by the endogenous inhibitor of protein phosphatase 2A (PP2A) I1PP2A in vitro.

in vivo

In vivo, memantine (2 mg/kg) restores PP2A activity, decreases GSK-3β and amyloid-β (Aβ) levels in the hippocampus, cerebral cortex, and ventricular areas, and attenuates spatial learning and memory in the AAV1-I1PP2A rat model of Alzheimer''s disease. Memantine (20 mg/kg) reduces responding on the ethanol-associated lever in a cue-induced ethanol-seeking test in rats. It also decreases secretion of matrix metalloproteinase-9 (MMP-9), degradation of collagen IV, the size of cerebral ischemia-induced brain infarcts, and neuronal cell death in a mouse model of focal cerebral ischemia.