Dizocilpine

Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a K_d of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca²⁺ flux^[1][2]. IC50 & Target:Ki: 37.2 nM (NMDA receptor, in rat brain membrane)^[1] In Vitro:Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg²⁺ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches^[3].
Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<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 create schizophrenia models. An intraperitoneal injection of 0.2 mg/kg in SD rats results in a half-life of 52.31 minutes, an AUC of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg^[2].