| Bioactivity | Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
| Target | Ki: 37.2 nM (NMDA receptor, in rat brain membrane) |
| Invitro | [3H]Dizocilpine maleate binds with NMDA receptor with a Kd 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 | Dizocilpine maleate (MK 801 maleate) (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 maleate (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine maleate (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 maleate (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]. |
| Name | Dizocilpine maleate |
| CAS | 77086-22-7 |
| Formula | C20H19NO4 |
| Molar Mass | 337.37 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Wong EH, et al. The anticonvulsant MK-801 is a potent N-Me-D-Asp antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8. [2]. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269. [3]. Huettner JE, et al. Block of N-Me-D-Asp-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85(4):1307-11. [4]. Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against neurotoxicity. Brain Res. 2005 Jul 19;1050(1-2):190-8. [5]. Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not for self-administration in rats. Learn Mem. 2008 Dec 2;15(12):857-65. [6]. Iijima Y, et al. Modification by MK-801 (dizocilpine), a noncompetitive NMDA receptor antagonist sensitization: evaluation by ambulation in mice. Nihon Shinkei Seishin Yakurigaku Zasshi. 1996 Feb;16(1):11-8. [7]. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-Me-D-Asp receptor activation. Neuroreport. 2017 May 24;28(8):444-450. |
Dizocilpine maleate
CAS: 77086-22-7 F: C20H19NO4 W: 337.37
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2
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