Memantine: Difference between revisions
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<StructureSection load='' size='340' side='right' caption=' | <StructureSection load='' size='340' side='right' caption='Memantine' scene='96/963765/Cv/1'> | ||
Memantine is a medication used to slow the progression of moderate-to-severe Alzheimer's disease. | Memantine is a medication used to slow the progression of moderate-to-severe Alzheimer's disease. It is believed to work by acting on NMDA receptors, working as pore blockers of these ion channels. See also [https://en.wikipedia.org/wiki/Memantine Memantine]. | ||
A dysfunction of glutamatergic neurotransmission, manifested as neuronal excitotoxicity, is hypothesized to be involved in the etiology of Alzheimer's disease. Targeting the glutamatergic system, specifically NMDA receptors, offers a novel approach to treatment in view of the limited efficacy of existing drugs targeting the cholinergic system. Memantine is a low-affinity voltage-dependent uncompetitive antagonist at glutamatergic NMDA receptors. By binding to the NMDA receptor with a higher affinity than Mg2+ ions, memantine is able to inhibit the prolonged influx of Ca2+ ions, particularly from extrasynaptic receptors, which forms the basis of neuronal excitotoxicity. The low affinity, uncompetitive nature, and rapid off-rate kinetics of memantine at the level of the NMDA receptor-channel, however, preserves the function of the receptor at synapses, as it can still be activated by physiological release of glutamate following depolarization of the postsynaptic neuron. | |||
<scene name='96/963765/Overall/1'>Memantine-bound GluN1a-GluN2B NMDA receptors</scene> ([[7sad]]); GluN1a subunits are in cyan, GluN2B subunits are in green, and memantine is in magenta. <scene name='96/963765/Binding_site/1'>Memantine binding site</scene>. | |||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Latest revision as of 17:02, 26 February 2024
Memantine is a medication used to slow the progression of moderate-to-severe Alzheimer's disease. It is believed to work by acting on NMDA receptors, working as pore blockers of these ion channels. See also Memantine. A dysfunction of glutamatergic neurotransmission, manifested as neuronal excitotoxicity, is hypothesized to be involved in the etiology of Alzheimer's disease. Targeting the glutamatergic system, specifically NMDA receptors, offers a novel approach to treatment in view of the limited efficacy of existing drugs targeting the cholinergic system. Memantine is a low-affinity voltage-dependent uncompetitive antagonist at glutamatergic NMDA receptors. By binding to the NMDA receptor with a higher affinity than Mg2+ ions, memantine is able to inhibit the prolonged influx of Ca2+ ions, particularly from extrasynaptic receptors, which forms the basis of neuronal excitotoxicity. The low affinity, uncompetitive nature, and rapid off-rate kinetics of memantine at the level of the NMDA receptor-channel, however, preserves the function of the receptor at synapses, as it can still be activated by physiological release of glutamate following depolarization of the postsynaptic neuron. (7sad); GluN1a subunits are in cyan, GluN2B subunits are in green, and memantine is in magenta. .
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