(-)MK-801 maleate

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

Product information

CAS Number: 121917-57-5

Molecular Weight: 337.37

Formula: C20H19NO4

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

Smiles: C[C@@]12N[C@@H](CC3=CC=CC=C13)C1=CC=CC=C21.OC(=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

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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).
2. 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.