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(+)MK-801 maleate — Datasheet

CAT. NO. DC7960

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ParameterValue
Chemical Name(-)-MK 801 Maleate
CAS No.77086-22-7
Synonyms(-)-MK 801 Maleate;(+)-MK 801 (hydrogen maleate);(+)-MK 801 Hydrogen;(+)-MK 801 hydrogen maleate;(+)-MK 801 MALEATE;(+)-MK 801 maleate (Dizocilpine);(+/-)-mk-801 hydrogen maleate;(+)-MK 801;Dizocilpine hydrogen maleate;Dizocilpine maleate;Dizocipine maleate;MK 801;(5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate;(5S)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-butenedioate;(-)-Dizocilpine (Maleate);EF13O02IV0;C13737;Dizocilpine maleate, (-)-;MLS000859982;HMS2097L12;HMS3714L12;HMS3675L08;HMS3411L08;HMS2233J12;HMS1570L12;2110AH;BN0339;s2857
FormulaC20H19NO4
M.Wt337.3692
SMILESO([H])C(/C(/[H])=C(/[H])\C(=O)O[H])=O.N1([H])[C@@]2([H])C([H])([H])C3=C([H])C([H])=C([H])C([H])=C3[C@]1(C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=C21
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

(+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

In Vitro

[3H]MK-801 binds with NMDA receptor with a Kd of 37.2 ±2.7 nM in rat cerebral cortical membranes[1]. MK-801 shows an inhibitory activity against N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50s of 20 nM and 9 nM, respectively[2]. MK-801 progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 blocks NMDA-activated single-channel activity in outside-out patches[3]. MK-801 (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells[4].

In Vivo

MK-801 (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice[4]. MK-801 (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement[5].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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