Dizocilpine (MK-801)

Description: Dizocilpine (MK-801), is a novel, potent, selective and non-competitive NMDA ( N-Methyl-D-aspartate) receptor antagonist with Kd of 37.2 nM in rat brain membranes. (+)-MK-801 blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. The drug acts as a potent anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions in test rats.

References: Proc Natl Acad Sci U S A. 1986 Sep; 83(18):7104-8; Eur J Pharmacol. 1988 Jan 12; 145(2):223-6.

Related CAS#?121917-57-5 (-)-MK-801; 77086-21-6 (free base)