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NMDA Antagonists
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There are eight medications with NMDA antagonism in clinical practice: ketamine, amantadine, memantine, methadone, dextromethorphan, Carbamazepine, phenytoin, and magnesium
Mechanism of NMDA Receptor Activation
The NMDA receptor is a complex ligand-gated and voltage-dependent ion channel. Its activation requires the simultaneous fulfillment of two conditions:
- Ligand Binding: The receptor must bind to the primary excitatory neurotransmitter, glutamate (typically binding to the NR2 subunit), and a co-agonist, which is usually glycine or D-serine (binding to the NR1 subunit).
- Sufficient Depolarization: The postsynaptic membrane potential must be sufficiently depolarized to relieve a voltage-dependent block imposed by magnesium ions.
Resources
NMDA antagonists - aiyer 2017.pdf - 4.4 MB (f)
