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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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Rats |
| Formulation | saline |
| Dosages | 0.20 mg/kg |
| Administration | i.p. |
| Molecular Weight | 337.37 |
| Formula | C20H19NO4 |
| CAS Number | 77086-22-7 |
| Solubility (25°C) | DMSO 100 mg/mL Water 6 mg/mL Ethanol 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NMDA Products |
|---|
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GluN1 (356-385) is an antigenic peptide against N-methyl-D-aspartate receptor (NMDAR) encephalitis. GluN1 (356-385) has the effect of reducing the density of surface NMDAR clusters in hippocampal neurons. |
| Glypromate acetate
Glypromate acetate 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. |
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