Dizocilpine

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Dizocilpine, also known as MK-801, is a non-competitive antagonist of the NMDA receptor, a type of glutamate receptor in the central nervous system. It is known for its role in neuroscience research and has been used extensively to study the pathophysiology of neurodegenerative diseases and neuroprotection.

Mechanism of Action

Dizocilpine binds to the NMDA receptor at the phencyclidine (PCP) site, blocking the flow of calcium ions through the ion channel. This inhibition prevents the excitotoxicity that can result from excessive glutamate activity, which is implicated in various neurological disorders.

Research Applications

Dizocilpine is widely used in preclinical research to investigate the role of NMDA receptors in synaptic plasticity, learning, and memory. It has also been employed in studies of stroke, traumatic brain injury, and schizophrenia.

Side Effects and Toxicity

Due to its potent effects on the central nervous system, dizocilpine can cause significant neurotoxicity and behavioral changes in animal models. These effects limit its potential for therapeutic use in humans.

See Also

• NMDA receptor antagonist
• Glutamate
• Neuroprotection
• Excitotoxicity
• Phencyclidine

External Links

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