(-)-Dizocilpine maleate_product_DataBase

Bioactivity	(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects[1][2].
Target	Ki: 211.7 nM (N-methyl-D-aspartate (NMDA) receptor)
Invitro	(-)-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]. Animal Model:
Name	(-)-Dizocilpine maleate
CAS	121917-57-5
Formula	C20H19NO4
Molar Mass	337.37
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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.

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