| CAS |
121917-57-5 |
| English Name |
(-)-MK 801 Maleate |
| Synonyms |
(-)-MK-801maleateGentisaldehyde |
| Molecular Formula |
C20H19NO4 |
| Molecular Weight |
337.37 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES |
C[C@@]1(N2)C3=CC=CC=C3C[C@H]2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O |
| InChIKey |
QLTXKCWMEZIHBJ-FWHYOZOBSA-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+;/m0./s1 |
| PubChem CID |
16219612 |
| Target Point |
iGluR;NMDA receptor |
| Passage |
Membrane Transporter&Ion Channel |
| Background |
(-)-MK 801 Maleate is a selective, selective, and non-competitive NMDA receptor antagonist. |
| Biological Activity |
(+)-MK-801 is known to be a specific non-competitive antagonist of N-methyl-D-aspartate (NMDA) receptors.Besides having an anticonvulsant effect， this compound possesses a central sympathomimetic effect and an anxiolytic-like action.[2] |
| IC50 |
Ki: 211.7nM(N-methyl-D-aspartate(NMDA) receptor)[1] |
| In Vitro |
(-)-Dizocilpine maleate((-)-MK-801 maleate)significantly inhibited the uptake of all three(norepinephrine，dopamine and serotonin)monoamine transporters in a dose-dependent manner in HEK cells. The Ki values of(-)-Dizocilpine on the norepinephrine，dopamine and serotonin transporters are 3.7 μM，40 μM and 47 μM，respectively[2]. |
| In Vivo |
(-)-Dizocilpine maleate(0.1 mg/kg; intraperitoneal injection; male adult C57BL/6 mice)treatment induces rapid antidepressant effects in the social defeat stress model[1]. |
| Data Literature Source |
[1]. Yang B，et al. Antidepressant Effects of (+)-MK-801 and (-)-MK-801 in the Social Defeat Stress Model. Int J Neuropsychopharmacol. 2016 Dec 30;19(12).
[2]. Nishimura M，et al. MK-801 blocks monoamine transporters expressed in HEK cells. FEBS Lett. 1998 Feb 27;423(3):376-80. |
| Unit |
Piece |
| Specification |
10mg 50mg |
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