Dizocilpine (maleate)

Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes. IC50 & Target:Ki: 37.2 nM (NMDA receptor, in rat brain membrane)^[1] In Vitro: [³H]Dizocilpine maleate binds with NMDA receptor with a K_d of 37.2±2.7 nM in rat cerebral cortical membranes^[1].
Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-Me-D-Asp^[3].
Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg²⁺ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine (MK-801) is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches^[3].
Dizocilpine maleate (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (MK-801; <500 μM) reduces microglial TNF-α output with an EC₅₀ of 400 μM in BV-2 cells^[4]. In Vivo: Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Dizocilpine maleate can be used to induce schizophrenia models. In SD rats, when administered intraperitoneally at a dose of 0.2 mg/kg, Dizocilpine maleate has a half-life of 52.31 minutes, an area under the curve (AUC) of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg^[2].