(-)-MK-801 (Dizocilpine, C13737) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
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Product Description
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(-)-MK-801 (Dizocilpine, C13737) is a potentN-methyl-D-aspartate (NMDA)receptor antagonist withKiof 30.5 nM. 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.
In vivo
All the control rats have severe permanent neurological deficits after ischemic spinal cord injury (ISCI), whereas the dizocilpine–treated rats have statistically (P < .05) better neurological outcome and good recovery. Histopathology reveals severe neuronal necrosis in the lumbar gray matter of control rats, whereas dizocilpine–treated rats show mild injury. These results demonstrate that a single dose of dizocilpine given before ISCI provides significant neuroprotection. Cell Data
cell lines：Caco-2, wild-type, and P-gp-overexpressing LLC-PK1
