PEAQX tetrasodium hydrate (Synonyms: NVP-AAM077 tetrasodium hydrate) |
Catalog No.GC36865
One-Click Copy Product Info
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PEAQX tetrasodium hydrate is a potent orally active NMDA antagonist, with IC50 values of 0.270μM for hNMDA 1A/2A and 29.6μM for 1A/2B receptors, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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PEAQX tetrasodium hydrate is a potent orally active NMDA antagonist, with IC50 values of 0.270μM for hNMDA 1A/2A and 29.6μM for 1A/2B receptors, respectively [1]. PEAQX tetrasodium hydrate is widely used in animal models to regulate motor ability and brain function[2].
In vitro, PEAQX tetrasodium hydrate treatment (5μM) for 5min inhibited Ca2+ influx induced by NMDA in rat primary neuronal cells [3]. Treatment with 3μM PEAQX tetrasodium hydrate for 12h induced apoptosis and increased caspase-3 levels in corticostriatal organotypic slice cultures[4].
In vivo, A single dose of 20mg/kg subcutaneous injection of PEAQX tetrasodium hydrate for 30min reduced the incidence of generalized seizures (GS) in a rat model of convulsive seizures[5]. A single subcutaneous injection of 3.75mg/kg PEAQX tetrasodium hydrate could improve the global social activities of adolescent male Sprague-Dawley rats within 2 days[6]. Subcutaneous injection of PEAQX tetrasodium hydrate (10mg/kg) twice daily for 14 days resulted in neonatal rats showing spatial working memory deficits as well as enhanced responsiveness to sound stimuli[7].
References:
[1] Auberson Y P, Allgeier H, Bischoff S, et al. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition[J]. Bioorganic & medicinal chemistry letters, 2002, 12(7): 1099-1102.
[2] Egunlusi A O, Joubert J. NMDA receptor antagonists: emerging insights into molecular mechanisms and clinical applications in neurological disorders[J]. Pharmaceuticals, 2024, 17(5): 639.
[3] Brittain M K, Brustovetsky T, Brittain J M, et al. Ifenprodil, a NR2B-selective antagonist of NMDA receptor, inhibits reverse Na+/Ca2+ exchanger in neurons[J]. Neuropharmacology, 2012, 63(6): 974-982.
[4] Anastasio N C, Xia Y, O'Connor Z R, et al. Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediating phencyclidine-induced perinatal neuronal apoptosis and behavioral deficits[J]. Neuroscience, 2009, 163(4): 1181-1191.
[5] Mares P, Tsenov G, Kubova H. Anticonvulsant action of GluN2A-preferring antagonist PEAQX tetrasodium hydrate in developing rats[J]. Pharmaceutics, 2021, 13(3): 415.
[6] Morales M, Varlinskaya E I, Spear L P. Low doses of the NMDA receptor antagonists, MK-801, PEAQX tetrasodium hydrate, and ifenprodil, induces social facilitation in adolescent male rats[J]. Behavioural brain research, 2013, 250: 18-22.
[7] Furuie H, Yamada M. Neonatal blockade of NR2A-containing but not NR2B-containing NMDA receptor induces spatial working memory deficits in adult rats[J]. Neuroscience Research, 2022, 176: 57-65.
| Cell experiment [1]: | |
Cell lines | Rat primary neuronal cells |
Preparation Method | Rat primary neuronal cells were maintained at 37°C in Earl's MEM with 5% CO2 supplemented with 10% NuSerum, 27mM glucose, and 26mM NaHCO3. Two 30-s pulses of NMDA (30μM, plus 10μM glycine) were used. PEAQX tetrasodium hydrate (5μM) was applied 5min before the second NMDA pulse, and the magnitude of the [Ca2+]c increase was compared with the [Ca2+]c increase in response to the first NMDA pulse. Ca2+ influx into neurons was assessed by measuring the magnitude of the [Ca2+]c increase. |
Reaction Conditions | 5µM; 5min |
Applications | PEAQX tetrasodium hydrate treatment resulted in inhibited Ca2+ influx induced by NMDA in cells. |
| Animal experiment [2]: | |
Animal models | Wistar-Imamichi rats |
Preparation Method | Wistar-Imamichi rats were subcutaneously injected with 10mg/kg PEAQX tetrasodium hydrate twice a day (at least 8 hours apart) from postnatal days 7 to 20. The rats were kept in a room with constant temperature and humidity, and the light-dark cycle of 12 hours (8:00 am to 8:00 pm). Food and water were allowed ad libitum, and behavioral phenotyping was performed thereafter. |
Dosage form | 10mg/kg; twice a day for 14 days; s.c. |
Applications | PEAQX tetrasodium hydrate treatment resulted in neonatal rats showing spatial working memory deficits as well as enhanced responsiveness to sound stimuli. |
References: | |
| Cas No. | SDF | ||
| Synonyms | NVP-AAM077 tetrasodium hydrate | ||
| Canonical SMILES | [O-]P([O-])(C(N[C@@H](C)C1=CC=C(Br)C=C1)C2=CC=CC3=C2N=C([O-])C([O-])=N3)=O.[H]O[H].[Na+].[Na+].[Na+].[Na+] | ||
| Formula | C17H15BrN3Na4O6P | M.Wt | 560.15 |
| Solubility | Water: 25.5 mg/mL (45.52 mM and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7852 mL | 8.9262 mL | 17.8524 mL |
| 5 mM | 357 μL | 1.7852 mL | 3.5705 mL |
| 10 mM | 178.5 μL | 892.6 μL | 1.7852 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)