Free shipping on all orders over $ 500

Dizocilpine maleate

Cat. No. M7581
Dizocilpine maleate Structure
Synonym:

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

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
10mg USD 51  USD51 In stock
50mg USD 183  USD183 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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 (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rats
Formulation saline
Dosages 0.20 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 337.37
Formula C20H19NO4
CAS Number 77086-22-7
Solubility (25°C) DMSO ≥ 90 mg/mL
Water 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Vojtechova I, et al. Behav Brain Res. Neonatal immune activation by lipopolysaccharide causes inadequate emotional responses to novel situations but no changes in anxiety or cognitive behavior in Wistar rats.

[2] Xu Y, et al. Sci Rep. In Vitro and In Vivo Characterization of PCC0104005, a Novel Modulator of Serotonin-Dopamine Activity, as an Atypical Antipsychotic Drug.

Related NMDA Products
Esketamine

Esketamine (ESK) is an NMDA-receptor antagonist.

Glypromate

Glypromate (Gly-Pro-Glu) is a neuroactive peptide with a potent action on acetylcholine release. Glypromate (Gly-Pro-Glu) is a weak NMDA receptor agonist binds to N-methyl-D-aspartate (NMDA) receptor with an IC50 value of 14.7 μM.

Radiprodil (RGH-896)

Radiprodil (also known as RGH-896) is an orally active and selective NMDA receptors antagonist which was evaluated as potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

Trans-crocetin

Trans-crocetin (Croceic Acid) is a blood-brain barrier-permeable NMDA receptor antagonist with high affinity, extracted from saffron (Crocus sativus L.). *The compound is unstable in solutions, freshly prepared is recommended

L-Glutamic acid monosodium salt hydrate

L-Glutamic acid monosodium salt hydrate is also a Kainate receptor, NMDA receptor and quisqualate receptor agonist; an excitatory amino acid neurotransmitter.

  Catalog
Abmole Inhibitor Catalog




Keywords: Dizocilpine maleate, Dizocilpine hydrogen maleate; (+)-MK 801 maleate; MK-801 maleate supplier, NMDA, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.