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(+)-MK 801 Maleate

Cat. No. M7581
(+)-MK 801 Maleate Structure
Synonym:

Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 190 In stock
100mg USD 320 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: [3H]MK-801 binds with NMDA receptor with a Kd of 37.2 ±2.7 nM in rat cerebral cortical membranes. 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. 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. 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.

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. 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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rats
Formulation saline
Dosages 0.20 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 337.37
Formula C20H19NO4
CAS Number 77086-22-7
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Neonatal immune activation by lipopolysaccharide causes inadequate emotional responses to novel situations but no changes in anxiety or cognitive behavior in Wistar rats.
Vojtechova I, et al. Behav Brain Res. 2018 May 2;349:42-53. PMID: 29729302.

In Vitro and In Vivo Characterization of PCC0104005, a Novel Modulator of Serotonin-Dopamine Activity, as an Atypical Antipsychotic Drug.
Xu Y, et al. Sci Rep. 2018 May 2;8(1):6892. PMID: 29720711.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: (+)-MK 801 Maleate, Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801 supplier, GluR, inhibitors

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