(+)-MK 801

Short Summary : Potent NMDA antagonist

Category : Membrane Transporter/Ion Channel|NMDA Receptor

Purity : 0.9905

CAS Number : 70449-94-4

Formula : C16H15N

Molecular Weight : 221.30

SMILE : C[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4

Solubility : >10.45mg/mL in DMSO

Storage : Store at -20°C

Description : (+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM [1].MK 801 is a potent anticonvulsant exhibits both anxiolytic and sympathomimetic properties. It is found to be a noncompetitive antagonist of NMDA. MK 801 can penetrate into the central nervous system. In the in vitro assay, MK 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner. This binding is reversible even when the concentration of MK 801 is up to 100M. It is also found that the binding shows a regional specificity. Most of these binding sites are located in the hippocampus. In rat cortical-slice preparations, MK 801 causes a potent blockade of depolarizing responses to NMDA with a high selectivity. This effect is persistent. The blockade can also cause a suppression of the epileptiform activity induced by tetrodotoxin or other neurotoxin [1].References:[1] Wong EH, Kemp JA, Priestley T, Knight AR, Woodruff GN, Iversen LL . The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.

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