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| Formula | C14H24N2O3 |
| Molar mass | 268.357 g·mol−1 |
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Nitromemantine (developmental code nameYQW-36) is a derivative ofmemantine developed in 2006 for the treatment ofAlzheimer's disease. It has been shown to reduceexcitotoxicity mediated by over-activation of theglutamatergic system, by blockingNMDA receptors.[1][2]
Like memantine, nitromemantine is a low-affinity voltage-dependentuncompetitiveantagonist at glutamatergic NMDA receptors, however nitromemantine selectively inhibitsextrasynaptic NMDA receptors while sparing normal physiological synaptic NMDA receptor activity, resulting in less side effects and a greater neuroprotective action, as well as stimulating regrowth of synapses with prolonged administration. The discoverers of nitromemantine have demonstrated that theamyloid-β peptide associated with Alzheimer's disease acts as an agonist atα7 nicotinic acetylcholine receptors, chronic overstimulation of which then results in uncontrolled release ofglutamate, and consequent excitotoxicity. By blocking extrasynaptic NMDA receptors, nitromemantine is able to largely prevent this excitotoxicity while minimising the side effects usually seen with less selective NMDA antagonists.[3] Thenitrate group of nitromemantine was found to bind to a second site on the extrasynaptic NMDA receptor which had previously been targeted withnitroglycerin, and this double action is thought to be responsible for the increased effectiveness of nitromemantine.[4]
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