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    Dizocilpine Maleate [(+)-MK 801 maleate]
    Dizocilpine Maleate [(+)-MK 801 maleate]

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1083
    CAS #: 77086-22-7Purity ≥98%

    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) 

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    Molecular Weight (MW)337.37
    CAS No.77086-22-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 68 mg/mL (201.6 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Other infoChemical Name: 5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate
    InChi Code: InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
    SMILES Code: CC1(N2)C3=CC=CC=C3CC2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
    SynonymsDizocilpine; MK801; MK 801; MK-801; MK 801 Maleate

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    In Vitro

    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.

    In Vivo(-)-Huperzine A can ameliorate the learning and memory deficiency in animal models and AD patients. Its potentially beneficial actions include modification of β-amyloid peptide processing, reduction of oxidative stress, neuronal protection against apoptosis, and regulation of the expression and secretion of nerve growth factor (NGF) and NGF signaling. (-)-Huperzine A significantly inhibits AChE activity in the cortex, hippocampus, striatum, medial septum, medulla oblongata, cerebellum, and hypothalamus of rats that are killed 30 min following the administration of (-)-Huperzine A at several dose levels compared with the saline control.
    Animal modelMale Sprague-Dawley rats
    Formulation & DosageDissolved in saline; 0.1mg/kg; oral gavage
    ReferencesProc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8; Eur J Pharmacol. 1988 Jan 12;145(2):223-6; Brain Res. 2005 Jul 19;1050(1-2):190-8; Learn Mem.2008 Dec 2;15(12):857-65.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    An external file that holds a picture, illustration, etc. Object name is nihms71896f4.jpg
    Differential MK-801 block and recovery of NMDA-eEPSCs and NMDA-mEPSCs.

    An external file that holds a picture, illustration, etc. Object name is nihms71896f1.jpg
    MK-801 block of NMDA-mEPSCs in hippocampal cultures.

    An external file that holds a picture, illustration, etc. Object name is nihms71896f9.jpg
    Asynchronous release detected in the absence of synaptotagmin 1 or in strontium is resistant to MK-801 application at rest.


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