dizocilpine

Dizocilpine (commonly known as MK-801) is a potent, selective, non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor—a subtype of glutamate receptor in the central nervous system. It acts as an open-channel blocker by binding within the NMDA-associated ion channel and preventing calcium influx. This blockade is use-dependent and voltage-dependent. Dizocilpine exhibits anticonvulsant and neuroprotective properties but is not used clinically due to its association with neurotoxicity (Olney's lesions), cognitive disruption, and psychotic-spectrum side effects in animal studies. It has also been shown to act as an antagonist at nicotinic acetylcholine receptors and can inhibit serotonin and dopamine transporters. Dizocilpine was discovered by Merck in 1982 and is widely used in research to model psychosis or study NMDA receptor function[1][2][3].

Other names

dizocilpine(+)-MK 801 maleate(-)-MK 801 maleatedizocilpine maleate