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 | |
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Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
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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 ≥ 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 |
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.
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