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Description: Dizocilpine Maleate [formerly (+)-MK-801)], the maleate salt of (+)dizocilpine, is a non-competitive antagonist of NMDA (N-Methyl-D-aspartate) receptors with a Kd of 37.2 nM in rat brain membranes. (+)-MK-801 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)
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: (-)-Huperzine A is a novel alkaloid isolated from the Chinese herb Huperzia serrata. (-)-Huperzine A preferentially inhibits tetrameric AChE (G4 form). (-)-Huperzine A is more potent than tacrine, physostigmine, galanthamine, and rivastigmine with respect to inhibition of AChE activity, whereas HupA is the least potent BuChE inhibitor among the inhibitors. (-)-Huperzine A possesses the ability to protect cells against hydrogen peroxide, β-amyloid protein, glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress, regulate the expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism.
Cell Assay: izocilpine ((+)-MK 801) (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.
Purity ≥98%
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