Dizocilpine maleate
Based on 49 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 77086-22-7
- Formula: C20H19NO4
- Molecular Weight:337.37
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neuroprotective Compound Library
HY-L070
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Ion Channel Compound Library
HY-L166
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) Dizocilpine maleate
More- Cell. 2023 Nov 22;186(24):5347-5362.e24. [Abstract]
- Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
- Nat Neurosci. 2022 Jan;25(1):39-49. [Abstract]
- Neuron. 2026 Apr 16:S0896-6273(26)00218-7. [Abstract]
- Mol Psychiatry. 2022 Sep;27(9):3885-3897. [Abstract]
- Alzheimers Res Ther. 2025 Dec 1;17(1):253. [Abstract]
- Cell Rep. 2026 Feb 18;45(3):117016. [Abstract]
- Cell Rep. 2026 Jan 3;45(1):116683. [Abstract]
- Brain Behav Immun. 2026 Jul:135:106529. [Abstract]
- Br J Pharmacol. 2020 Oct;177(20):4720-4733. [Abstract]
- J Med Chem. 2026 Feb 10. [Abstract]
- J Med Chem. 2023 May 11;66(9):6274-6287. [Abstract]
- Virulence. 2025 Dec;16(1):2490208. [Abstract]
- Cell Biosci. 2023 Mar 16;13(1):57. [Abstract]
- Life Sci. 2022 Apr 15:295:120419. [Abstract]
- RSC Adv. 2022 Oct 3;12(43):28098-28103. [Abstract]
- Eur J Pharmacol. 2022 Dec 5:936:175343. [Abstract]
- Eur J Pharmacol. 2019 Aug 15:857:172427. [Abstract]
- Int J Mol Sci. 2022 Dec 18;23(24):16150. [Abstract]
- Mol Neurobiol. 2026 Jun 24;63(1):716. [Abstract]
- Food Safety and Health. 2026 Jan 7.
- Mol Neurobiol. 2024 Jul;61(7):4166-4177. [Abstract]
- Front Cell Dev Biol. 2020 Feb 4:8:24. [Abstract]
- Chem Biol Interact. 2026 Apr 28:112112. [Abstract]
- Molecules. 2023 Mar 2;28(5):2304. [Abstract]
- Sci Rep. 2025 May 25;15(1):18255. [Abstract]
- Neuropharmacology. 2025 May 1:268:110318. [Abstract]
- Neuropharmacology. 2025 Mar 15:266:110284. [Abstract]
- J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]
- J Physiol. 2023 Aug;601(16):3585-3604. [Abstract]
- Front Cell Neurosci. 2019 Jun 25:13:276. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2025 Dec 20:143:111555. [Abstract]
- Front Biosci (Landmark Ed). 2023 Jul 19;28(7):140. [Abstract]
- Front Neurosci. 2019 Nov 19:13:1225. [Abstract]
- J Orthop Surg Res. 2025 Jan 23;20(1):83. [Abstract]
- Bioorg Med Chem. 2022 Apr 1:59:116675. [Abstract]
- Psychoneuroendocrinology. 2024 Oct:168:107138. [Abstract]
- Psychopharmacology (Berl). 2025 Mar;242(3):651-661. [Abstract]
- Brain Res. 2023 Aug 1:1812:148409. [Abstract]
- Cell Tissue Res. 2026 Jun 24;405(1):3. [Abstract]
- Behav Brain Res. 2026 Apr 27:510:116247. [Abstract]
- Behav Brain Res. 2026 Feb 26:498:115917. [Abstract]
- Eur J Neurosci. 2024 Sep;60(5):4830-4842. [Abstract]
- Neurosci Lett. 2023 Sep 25:814:137471. [Abstract]
- Neuroreport. 2017 May 24;28(8):444-450. [Abstract]
- Basic Clin Neurosci. 2023 Jan-Feb;14(1):103-116. [Abstract]
- SSRN. 2025 Jun 18.
- Res Sq. 2024 Jul 15.
- Evid Based Complement Alternat Med. 2020 Mar 10:2020:3524641. [Abstract]
Customer Validation & Images
-
Cell Migration/Invasion Assay
-
Flow Cytometry
-
WB
-
In Vivo Efficacy Study
-
Histological Imaging/Staining
All iGluR Isoforms
More
Biological Activity
|
NMDA Receptor |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
7.91 nM
Compound: MK-801
|
Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay
Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay
|
[PMID: 23033965] |
[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 induce schizophrenia models. In SD rats, when administered intraperitoneally at a dose of 0.2 mg/kg, Dizocilpine maleate has a half-life of 52.31 minutes, an area under the curve (AUC) of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg[2].
Administration: 0.4 mg/kg • i.p. • single dose.
Prepulse Inhibition (PPI): Decreased PPI significantly.
maze test:Avoided open arm entries in elevated plus maze test and reduced number of novel arm entries in Y maze test.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 77086-22-7
-
Appearance Solid
-
Molecular Weight 337.37
-
Formula C20H19NO4
-
Color White to off-white
-
SMILES
C[C@]12C3=CC=CC=C3C[C@@H](N2)C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
-
Synonyms
(+)-MK 801 Maleate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (49)
-
Journal Impact Factor
-
Most Recent
-
Cell
2023 Nov 22;186(24):5347-5362.e24. PMID: 37963465 -
Sci Bull
Tumor cell-derived N-acetyl-aspartyl-glutamate reshapes the tumor microenvironment to facilitate breast cancer metastasis. [Abstract]2025 Apr 15;70(7):1126-1138. PMID: 39800628
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
The invasion assay was conducted using SUM159 cells (left) or 4T1 cells (right) treated with NAAG, MK801 (100 μM), or the combination.
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
BMCs were treated with NAAG, MK801 (100 μM), or the combination for 5 d. The PMN-MDSC percentages in BMCs were analyzed using flow cytometry.
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
BMCs were treated with NAAG, MK801 (100 μM), or the combination for 5 d. The cells were collected and lysed for Western blotting to detect ARG1 expression.
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
The tumor growth curve of 4T1 allograft mice treated with NAAG, MK801 (i.p., 1 mg/kg, 5 d a week), or the combination (n = 6).
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138. [Abstract]
HE staining of lungs from 4T1 tumor-bearing mice treated with NAAG, MK801 (i.p., 1 mg/kg, 5 d a week), or the combination. Representative images (left) and a bar graph (right) were shown. Scale bar, 200 μm.
-
Nat Neurosci
Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties. [Abstract]2022 Jan;25(1):39-49. PMID: 34887590 -
Neuron
2026 Apr 16:S0896-6273(26)00218-7. PMID: 41997149 -
Mol Psychiatry
2022 Sep;27(9):3885-3897. PMID: 35715487 -
Alzheimers Res Ther
Ceftriaxone alleviates mitochondrial damage through the inhibition of extrasynaptic NMDA receptor-mediated changes in intracellular calcium levels to improve cognitive deficits in APP/PS1 mice. [Abstract]2025 Dec 1;17(1):253. PMID: 41327376 -
Cell Rep
PCIF1-mediated m6Am modification in ACC neurons participates in inflammatory pain and anxiety. [Abstract]2026 Feb 18;45(3):117016. PMID: 41712381 -
Cell Rep
Macrophage glycine transporter supports IL-1β production by modulating the AKT1/mTOR/NLRP3 pathway. [Abstract]2026 Jan 3;45(1):116683. PMID: 41485223 -
Brain Behav Immun
NR2B-CaMKII signaling in the dentate gyrus driven by astrocytic P2Y1Rs mediates the antidepressant effect of low-dose LPS. [Abstract]2026 Jul:135:106529. PMID: 41796645 -
Br J Pharmacol
Prefrontal inhibition of neuronal Kv 7 channels enhances prepulse inhibition of acoustic startle reflex and resistance to hypofrontality. [Abstract]2020 Oct;177(20):4720-4733. PMID: 32839968 -
J Med Chem
Bioisostere-Driven Discovery of SePP: A Selenium-Containing Polypharmacological Agent Relevant to Fragile X Syndrome. [Abstract]2026 Feb 10. PMID: 41666325 -
J Med Chem
Transformation of a Dopamine D2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents. [Abstract]2023 May 11;66(9):6274-6287. PMID: 37130037 -
Virulence
2025 Dec;16(1):2490208. PMID: 40202859 -
Cell Biosci
Remote ischemic preconditioning protects against spinal cord ischemia-reperfusion injury in mice by activating NMDAR/AMPK/PGC-1α/SIRT3 signaling. [Abstract]2023 Mar 16;13(1):57. PMID: 36927808
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2023 Mar 16;13(1):57. [Abstract]
Dizocilpine (MK-801; 1 mg/kg; i.v.; single) suppresses RIPC-induced SIRT3 upregulation in mice.
-
Life Sci
EphrinB2/ephB2 activation facilitates colonic synaptic potentiation and plasticity contributing to long-term visceral hypersensitivity in irritable bowel syndrome. [Abstract]2022 Apr 15:295:120419. PMID: 35183555 -
RSC Adv
Polyphosphoric acid-promoted one-pot synthesis and neuroprotective effects of flavanones against NMDA-induced injury in PC12 cells. [Abstract]2022 Oct 3;12(43):28098-28103. PMID: 36320275 -
Eur J Pharmacol
Chemerin-9 in paraventricular nucleus increases sympathetic outflow and blood pressure via glutamate receptor-mediated ROS generation. [Abstract]2022 Dec 5:936:175343. PMID: 36306926 -
Eur J Pharmacol
2019 Aug 15:857:172427. PMID: 31152702 -
Int J Mol Sci
Neuroprotection of Kaji-Ichigoside F1 via the BDNF/Akt/mTOR Signaling Pathways against NMDA-Induced Neurotoxicity. [Abstract]2022 Dec 18;23(24):16150. PMID: 36555790 -
Mol Neurobiol
Desloratadine Rescues Schizophrenia-like Phenotypes by Inhibiting the Pathogenic 5-HT2AR-PI3K/AKT/mTOR Signaling Axis. [Abstract]2026 Jun 24;63(1):716. PMID: 42340538 -
-
Mol Neurobiol
Inhibiting Caveolin-1-Related Akt/mTOR Signaling Pathway Protects Against N-methyl-D-Aspartate Receptor Activation-Mediated Dysfunction of Blood-Brain Barrier in vitro. [Abstract]2024 Jul;61(7):4166-4177. PMID: 38066401 -
Front Cell Dev Biol
Parvalbumin Interneuron Activation-Dependent Adult Hippocampal Neurogenesis Is Required for Treadmill Running to Reverse Schizophrenia-Like Phenotypes. [Abstract]2020 Feb 4:8:24. PMID: 32117963 -
Chem Biol Interact
A novel HDAC1-Hcy/Glu-ferroptosis axis underlies valproic acid-induced hepatic steatosis. [Abstract]2026 Apr 28:112112. PMID: 42061694 -
Molecules
2023 Mar 2;28(5):2304. PMID: 36903552 -
Sci Rep
ZD7288 ameliorates long-term cerebral ischemia reperfusion-induced deterioration of spatial memory by regulating the expressions of NMDA receptor subunits in rats. [Abstract]2025 May 25;15(1):18255. PMID: 40415080 -
Neuropharmacology
MK-801 attenuates one-trial tolerance in the elevated plus maze via the thalamic nucleus reuniens. [Abstract]2025 May 1:268:110318. PMID: 39842626 -
Neuropharmacology
Curcumin analog C16 attenuates bone cancer pain induced by MADB 106 breast cancer cells in female rats and inhibits the CREB/NLGN2 signaling axis by targeting CaMKⅠα. [Abstract]2025 Mar 15:266:110284. PMID: 39725125 -
J Cell Mol Med
Calpain-2 plays a pivotal role in the inhibitory effects of propofol against TNF-α-induced autophagy in mouse hippocampal neurons. [Abstract]2020 Aug;24(16):9287-9299. PMID: 32627970
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]
Neurons are pre-treated with 10 μM Dizocilpine (MK801), followed by TNF-α treatment (40 ng/mL, 2 h). MK801 could attenuate TNF-α- induced intracellular calcium accumulation, phosphorylation of CAMK II and calpain-2, calpain activation and cathepsin B release as well as TrkB truncation.
-
J Physiol
Orexin recruits non-selective cationic conductance and endocannabinoid to dynamically modulate firing of caudal pontine reticular nuclear neurones. [Abstract]2023 Aug;601(16):3585-3604. PMID: 37421377 -
Front Cell Neurosci
Pin1 Is Regulated by CaMKII Activation in Glutamate-Induced Retinal Neuronal Regulated Necrosis. [Abstract]2019 Jun 25:13:276. PMID: 31293391 -
Prog Neuropsychopharmacol Biol Psychiatry
Clozapine mitigates MK-801-induced mismatch negativity impairment in a rat electroencephalography study: relevance for schizophrenia drug development. [Abstract]2025 Dec 20:143:111555. PMID: 41187893 -
Front Biosci (Landmark Ed)
A Metabolomics-Based Study on NMDAR-Mediated Mitochondrial Damage through Calcium Overload and ROS Accumulation in Myocardial Infarction. [Abstract]2023 Jul 19;28(7):140. PMID: 37525913 -
Front Neurosci
High-Frequency Repetitive Transcranial Magnetic Stimulation Mediates Autophagy Flux in Human Bone Mesenchymal Stromal Cells via NMDA Receptor-Ca2+-Extracellular Signal-Regulated Kinase-Mammalian Target of Rapamycin Signaling. [Abstract]2019 Nov 19:13:1225. PMID: 31798406 -
J Orthop Surg Res
Activation of osteoblast ferroptosis by risperidone accelerates bone loss in mice models of schizophrenia. [Abstract]2025 Jan 23;20(1):83. PMID: 39849573 -
Bioorg Med Chem
Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells. [Abstract]2022 Apr 1:59:116675. PMID: 35202968 -
Psychoneuroendocrinology
Chronic intranasal oxytocin alleviates cognitive impairment and reverses oxytocin signaling upregulation in MK801-induced mice. [Abstract]2024 Oct:168:107138. PMID: 39068687 -
Psychopharmacology (Berl)
Efficacy and safety of prophylactic use of benzhexol after risperidone treatment in MK-801-induced mouse model of schizophrenia. [Abstract]2025 Mar;242(3):651-661. PMID: 39551830 -
Brain Res
Inhibition of glycolysis prevents behavioural changes in mice with MK801-induced SCZ model by alleviating lactate accumulation and lactylation. [Abstract]2023 Aug 1:1812:148409. PMID: 37207839 -
Cell Tissue Res
Cardiac α2δ1 C-terminal contributes to left atrial hypertrophy in chronic ischemic heart failure, in association with changes in membrane GluN1 and p-CAMKII/p-HDAC4 signaling. [Abstract]2026 Jun 24;405(1):3. PMID: 42337146 -
Behav Brain Res
Gamma-band transcranial alternating current stimulation restores motor function in a Parkinson's disease mouse model. [Abstract]2026 Apr 27:510:116247. PMID: 42055168 -
Behav Brain Res
Mechanistic study of platelet-derived exosome-mediated miR-320a on attenuation of schizophrenia-like behavior in rat models via ITGβ modulation. [Abstract]2026 Feb 26:498:115917. PMID: 41202989 -
Eur J Neurosci
Chemerin in caudal division of nucleus tractus solitarius increases sympathetic activity and blood pressure. [Abstract]2024 Sep;60(5):4830-4842. PMID: 39044301 -
Neurosci Lett
Inhibition of neuronal Kv7 channels ameliorates MK-801-induced cognitive dysfunction in mice via up-regulating NAMPT expression. [Abstract]2023 Sep 25:814:137471. PMID: 37673371 -
Neuroreport
Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-methyl-D-aspartate receptor activation. [Abstract]2017 May 24;28(8):444-450. PMID: 28394782
Dizocilpine maleate purchased from MedChemExpress. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450. [Abstract]
Western blot analysis confirms that MK-801 inhibits the decrease in GDF10 in SNL rats. The relative expression level of GDF10 in the SNL-vehicle group is significantly decreased, but remains unchanged in the SNL-MK-801 group versus sham.
-
Basic Clin Neurosci
Datumetine Preferentially Upregulates N-methyl-D-aspartate Receptor Signalling Pathways in Different Brain Regions of Mice. [Abstract]2023 Jan-Feb;14(1):103-116. PMID: 37346877 -
-
-
Evid Based Complement Alternat Med
Acupuncture at Gastric Back-Shu and Front-Mu Acupoints Enhances Gastric Motility via the Inhibition of the Glutamatergic System in the Hippocampus. [Abstract]2020 Mar 10:2020:3524641. PMID: 32215036
Solvent & Solubility
DMSO : 133.33 mg/mL (395.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 25 mg/mL (74.10 mM; Need ultrasonic)
H2O : 7.69 mg/mL (22.79 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.19 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.19 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Saline
Solubility: 3.45 mg/mL (10.23 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Animals are given saline or Dizocilpine ((+)-MK 801) followed by cocaine 30 min later in the home cage instead of in the CPP apparatus for the two days of “reactivation.” This is done to determine whether reactivation of the memory for the cocaine-associated context by cocaine in the CPP context is necessary for the ability of Dizocilpine ((+)-MK 801) to disrupt reconsolidation. Animals undergo preconditioning, conditioning, testing, and extinction but animals are injected with saline or Dizocilpine ((+)-MK 801) (0.20 mg/kg, i.p.) 30 min prior to a cocaine injection (10 mg/kg, i.p.) in the home cage. Animals remain in the home cages, and the next day, the procedure from the first day of reactivation is repeated. The following day, animals are tested for cocaine-primed reinstatement in their CPP box without any prior microinjection of saline or Dizocilpine ((+)-MK 801).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (293 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
References
[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]. Wegener N, et al. Evaluation of brain pharmacokinetics of (+)MK-801 in relation to behaviour. Neurosci Lett. 2011 Sep 26;503(1):68-72. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / Ethanol / DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| Ethanol / DMSO | 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| DMSO | 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Dizocilpine maleate Related Classifications
HY-15084 Related Classifications
Powered by Bioz