Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitiveNMDA receptorantagonist, with aK_dof 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].

Ki: 37.2 nM (NMDA receptor, in rat brain membrane)^[1]

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 reduces microglial tnf-α output an ec₅₀of 400 μM in BV-2 cells^[4].

Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice^[4].
Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (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^[5].
Dizocilpine (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg^[6].

221.30

C₁₆H₁₅N

77086-21-6

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