Dizocilpine (MK-801), is a non-competitive antagonist of the N-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor. Glutamate is the brain's primary excitatory neurotransmitter. The channel is normally blocked with a magnesium ion and requires depolarization of the neuron to remove the magnesium and allow the glutamate to open the channel, causing an influx of calcium, which then leads to subsequent depolarization. MK-801 binds inside the ion channel of the receptor at several of PCP's binding sites thus preventing the flow of ions, including an influx of calcium (Ca2+), through the channel. Dizocilpine blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it.However, dizocilpine is the most frequently used non-competitive NMDA receptor antagonist in animal models to mimic psychosis for experimental purposes.
-O641.gif)