Cat No.: 77086-22-7
Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM
IC50 Value: 30.5 nM.
NMDA (N-methyl-D-aspartate) receptor antagonist (MK-801) were used to treat hyperalgesia in the diabetic neuropathic pain (DNP).
in vitro: Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrates a potent, selective, and noncompetitive antagonistic action of dizocilpine on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate. The potencies of phencyclidine, ketamine, SKF 10047, and the enantiomers of dizocilpine as N-Me-D-Asp antagonists correlate closely (r = 0.99) with their potencies as inhibitors of [3H] dizocilpine binding. This suggests that the dizocilpine binding sites are associated with N-Me-D-Asp receptors and provides an explanation for the mechanism of action of dizocilpine as an anticonvulsant. The cytotoxicity of MK-801 on cultured microglia was also investigated. Cytotoxicity of MK-801 was reduced by t...
Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
References: for more information, please visit http://www.ncbi.nlm.nih.gov