| CAS |
77086-22-7 |
| Chinese Name |
(+)-MK 801 顺丁烯二酸盐 |
| English Name |
(+)-MK 801 Maleate |
| Synonyms |
Dizocilpine maleate;地卓亚平马来酸盐;MK-801 maleate |
| Molecular Formula |
C20H19NO4 |
| Molecular Weight |
337.37 |
| Solubility |
Soluble in DMSO |
| Purity |
≥99% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 278-614-5 |
| MDL |
MFCD00082465 |
| SMILES |
C[C@]12C3=CC=CC=C3C[C@@H](N2)C4=CC=CC=C14.O=C(O)/C=C\C(O)=O |
| InChIKey |
QLTXKCWMEZIHBJ-PJGJYSAQSA-N |
| InChI |
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-/t15-,16+;/m1./s1 |
| PubChem CID |
6420042 |
| Target Point |
iGluR |
| Passage |
Membrane Transporter&Ion Channel |
| Background |
(+)-MK 801 Maleate is a potent, selective, non-competitive NMDA receptor antagonist. |
| Biological Activity |
Dizocilpine maleate (MK-801 maleate) is a potent， selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.[1] |
| IC50 |
Ki: 37.2nM(NMDA receptor，in rat brainmembrane)[1] |
| In Vitro |
[3H]Dizocilpine maleate binds with NMDA receptor with a Kd of 37.2±2.7 nM in rat cerebral cortical membranes[1].Dizocilpine maleate(< 500 μM)inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine(MK-801; <500 μM)reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells[2]. |
| In Vivo |
Dizocilpine maleate(MK 801 maleate)(1 mg/kg)treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine(MK 801)(1 mg/kg)also attenuates the effects of METH on microglial activation in striatal of mice[2]. |
| Data Literature Source |
[1]. Wong EH，et al. The anticonvulsant MK-801 is a potent N-Me-D-Asp antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.
[2]. Thomas DM，et al. MK-801 and dextromethorphan block microglial activation and protect against neurotoxicity. Brain Res. 2005 Jul 19;1050(1-2):190-8. |
| Unit |
Bottle |
| Specification |
10mg 10 mM * 1 mL in DMSO 50mg |
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