(-)MK-801 maleate

Cas：121917-57-5

Product Information：

(-)MK-801 maleate is a noncompetitive antagonist of the NMDA receptor, as a less active enantiomer.

Chemical Formula: C20H19NO4

Exact Mass: 337.1314

Molecular Weight: 337.38

Elemental Analysis: C, 71.20; H, 5.68; N, 4.15; O, 18.97

Synonym: 

(-)-MK 801 hydrogen maleate

(-)-MK 801 Maleate

(-)-MK 801 (Maleate)

Chemical Name: (5R,10S)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate

InChi Key:

QLTXKCWMEZIHBJ-FWHYOZOBSA-N

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-/t15-,16+;/m0./s1

Smiles Code:

C[C@@]1(N2)C3=CC=CC=C3C[C@@]2([H])C4=CC=CC=C14.O=C(O)/C=C\C(O)=O

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

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.

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.

References：

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).

1. Nishimura M, et al. MK-801 blocks monoamine transporters expressed in HEK cells. FEBS Lett. 1998 Feb 27;423(3):376-80.

Products are for research use only. Not for human use.