Dizocilpine maleate (Synonyms: 地卓亞平馬來酸鹽; MK-801 maleate)
Dizocilpine maleate (MK-801 maleate) 是一種有效，選擇性，非競爭性的 NMDA 受體拮抗劑，Kd 值為 37.2 nM。
生物活性
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.
IC50 & Target
Ki: 37.2 nM (NMDA receptor, in rat brain membrane)[1]
體外研究(In Vitro)
[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].
體內(nèi)研究(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].
分子量：337.37
性狀：Solid
Formula：C20H19NO4
CAS 號：77086-22-7
中文名稱：地卓亞平馬來酸鹽
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數(shù)據(jù)
DMSO : 133.33 mg/mL (395.20 mM; Need ultrasonic)
Ethanol : 25 mg/mL (74.10 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： Saline
Solubility: 3.45 mg/mL (10.23 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.19 mg/mL (6.49 mM); Clear solution
- 5.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution
- 6.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution
參考文獻(xiàn)
[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. [Content Brief]
[2]. Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
注：產(chǎn)品僅用于科研
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