tcsc1290 Dizocilpine (Maleate)

Dizocilpine ((+)-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]MK-801 binds with NMDA receptor with a K_d of 37.2 ±2.7 nM in rat cerebral cortical membranes^[1]. Dizocilpine ((+)-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^[2]. Dizocilpine ((+)-MK 801) progressively suppresses of current induced by NMDA. Mg²⁺ (10 mM) prevents Dizocilpine ((+)-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^[3]. Dizocilpine ((+)-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^[4].

In Vivo: 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].