Memantine hydrochloride

Memantine is an uncompetitive NMDA receptor antagonist. When using HEK293 cells express recombinant rat NMDA receptors, memantine shows inhibition of L-glutamate-mediated response with a dose- and voltage-dependent manner. Memantine also has a rapid unblocking kinetics. Memantine is used clinically in spasticity, Parkinson's disease and Alzheimer's disease. Memantine is found to attenuate the deleterious action of Aβ in the in vitro numerous studies. It is probably due to the decreased tau phosphorylation caused by memantine. (In Vitro) :Memantine (hydrochloride) (D-145 (hydrochloride) ) is a moderate-affinity, uncompetitive, voltage-dependent, NMDA-receptor antagonist with fast on/off kinetics that inhibits excessive calcium influx induced by chronic overstimulation of the NMDA receptor. Memantine is approved in the US and the EU for the treatment of patients with moderate to severe dementia of the Alzheimer's type. Memantine has considerable therapeutic potential for the myriad of clinical entities associated with NMDA receptor-mediated neurotoxicity. Memantine blocked 200 microM NMDA-evoked responses with a 50% inhibition constant (IC50) of approximately 1 microM at -60 mV and an empirical Hill coefficient of approximately.