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- Alomone Labs Memantine hydrochloride inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes.A. Time course of NMDA currents elicited 100 µM glutamate every 50s, while membrane potential was held at -80 mV. 1 and 10 µM Memantine hydrochloride (#M-145), applied for 2 min each, as indicated, reversibly inhibited current amplitude. B. superimposed current traces taken from the experiment described in A.
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Memantine, a derivative of amantadine, is a low-affinity, voltage-dependent, non-competitive N-methyl-D-aspartate (NMDA) antagonist with strong voltage dependency and rapid unblocking kinetics. Memantine acts on activated NMDA receptor by binding to a site located in the channel of the receptor and inhibiting the Ca2+ influx. Its IC50 value is around 1 µM at -70 mV5.
Memantine has neuroprotective effects, preventing glutamatergic over-stimulation and the neurotoxicity caused by it by decreasing glutamate excitotoxicity. In rats, memantine shows increased levels of brain-derived neurotrophic factor (BDNF) thus influencing synaptic plasticity, β-amyloid-induced apoptotic death and neuroinflammation in the hippocampus1.
Proper NMDA function is required for synaptic plasticity. NMDA receptors can be found in dendrites of pyramidal cells in the hippocampus and cortex.
Memantine is currently in clinical use for treatment of Alzheimer´s disease symptoms with significant benefits on cognitive, functional, and general status2. The drug is well tolerated with fast course of action and uncommon adverse effects such as: dizziness, confusion, somnolence, hallucinations, and nausea which disappear after discontinuation or dose reduction3.
Some studies have suggested to considering administration of memantine in the treatment of bipolar disorders that do not respond to standard mood stabilizers4.
Memantine hydrochloride (#M-145) is a highly pure, synthetic, and biologically active compound.