PEAQX tetrasodium hydrate
(Synonyms: NVP-AAM077 tetrasodium hydrate) 目录号 : GC36865
PEAQX tetrasodium hydrate是一种强效且有口服活性的NMDA受体拮抗剂，对hNMDA 1A/2A和1A/2B受体的IC50值分别为0.270μM和29.6μM。
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.
PEAQX tetrasodium hydrate是一种强效且有口服活性的NMDA受体拮抗剂，对hNMDA 1A/2A和1A/2B受体的IC50值分别为0.270μM和29.6μM[1]。PEAQX tetrasodium hydrate广泛应用于动物模型中调节运动能力和脑功能[2]。
在体外，5μM的PEAQX tetrasodium hydrate处理大鼠原代神经元细胞5分钟可抑制NMDA诱导的Ca2+内流[3]。3μM的PEAQX tetrasodium hydrate处理皮质纹状体器官型脑片培养物12小时能诱导细胞凋亡并增加caspase-3水平[4]。
在体内，惊厥发作大鼠模型单次皮下注射20mg/kg剂量的PEAQX tetrasodium hydrate（30分钟）可降低全身性癫痫发作发生率[5]。青春期雄性Sprague-Dawley大鼠单次皮下注射3.75mg/kg剂量的PEAQX tetrasodium hydrate能在2天内改善整体社交活动[6]。新生大鼠每日两次皮下注射10mg/kg的PEAQX tetrasodium hydrate（持续14天）会导致空间工作记忆缺陷并增强对声音刺激的反应性[7]。
| 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 | ||
| 别名 | 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+] | ||
| 分子式 | C17H15BrN3Na4O6P | 分子量 | 560.15 |
| 溶解度 | Water: 25.5 mg/mL (45.52 mM and warming) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet