Memantine hydrochloride
(Synonyms: 盐酸美金刚; D-145 hydrochloride) 目录号 : GC10198
Memantine hydrochloride是一种非竞争性N-甲基-D-天冬氨酸受体（NMDAR）拮抗剂，IC50值为0.5-1μM。
Cas No.:41100-52-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Memantine hydrochloride is a non-competitive N-methyl-D-aspartate receptor (NMDAR) antagonist, with the IC50 values of 0.5-1μM[1]. Memantine hydrochloride protects neurons against toxicity caused by overactivation of NMDAR and blocks the effects of tonic pathologically elevated levels of glutamate that may lead to neuronal dysfunction[2]. Memantine hydrochloride has been used in animal models to treat various types of dementia and neurodegenerative diseases[3].
In vitro, Memantine hydrochloride treatment at 50μM for 24 hours significantly alleviated the decrease in rat hippocampal cell viability induced by amyloid protein β1-42, increased the number of living cells, and enhanced cell viability[4]. Treatment with 10μM Memantine hydrochloride for 6 hours attenuated the oxidative stress induced by oxygen-glucose deprivation/reperfusion in human umbilical vein endothelial cells (HUVECs), increased the expression of Nrf2 and HO-1, and enhanced cell viability[5]. Treatment with 250μM Memantine hydrochloride for 48 hours resulted in a significant increase in the expression level of the pro-apoptotic protein Bax in LNCaP cells, and induced cell cycle arrest at the G0/G1 phase[6].
In vivo, Memantine hydrochloride treatment (20mg/kg) by gavage daily for 2 months can improve the spatial learning ability of APP/PS1 mice and alleviate memory impairment[7]. Continuous intraperitoneal injection of 10mg/kg/day dose of Memantine hydrochloride for 10 consecutive days could alleviate the parasitemia in BALB/c mice infected with Trypanosoma cruzi, resulting in a reduction in cardiac parasitic load and inflammatory infiltration, and an increase in the survival rate of the mice[8].
References:
[1] Kotermanski S E, Johnson J W. Mg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine[J]. Journal of Neuroscience, 2009, 29(9): 2774-2779.
[2] Witt A, Macdonald N, Kirkpatrick P. Memantine hydrochloride[J]. Nature reviews Drug discovery, 2004, 3(2): 109-110.
[3] Peng D, Yuan X, Zhu R. Memantine hydrochloride in the treatment of dementia subtypes[J]. Journal of Clinical Neuroscience, 2013, 20(11): 1482-1485.
[4] Rozumna N M, Hanzha V V, Lukyanetz E A. Memantine protects the cultured rat hippocampal neurons treated by NMDA and amyloid β1–42[J]. Frontiers in Neuroscience, 2023, 17: 1269664.
[5] Lv X, Li Q, Mao S, et al. The protective effects of memantine against inflammation and impairment of endothelial tube formation induced by oxygen-glucose deprivation/reperfusion[J]. Aging (Albany NY), 2020, 12(21): 21469.
[6] Albayrak G, Konac E, Dikmen A U, et al. Memantine induces apoptosis and inhibits cell cycle progression in LNCaP prostate cancer cells[J]. Human & experimental toxicology, 2018, 37(9): 953-958.
[7] Li P, Xu J, Gu H, et al. Memantine ameliorates cognitive deficit in AD mice via enhancement of entorhinal–CA1 projection[J]. BMC neuroscience, 2021, 22(1): 41.
[8] Santos Souza H F, Rocha S C, Damasceno F S, et al. The effect of memantine, an antagonist of the NMDA glutamate receptor, in in vitro and in vivo infections by Trypanosoma cruzi[J]. PLoS neglected tropical diseases, 2019, 13(9): e0007226.
Memantine hydrochloride是一种非竞争性N-甲基-D-天冬氨酸受体（NMDAR）拮抗剂，IC50值为0.5-1μM[1]。Memantine hydrochloride通过保护神经元免受NMDAR过度激活引起的毒性作用，并阻断病理性升高的谷氨酸水平导致的神经元功能障碍[2]。Memantine hydrochloride已广泛应用于多种痴呆和神经退行性疾病动物模型的治疗研究[3]。
在体外，50μM 的Memantine hydrochloride处理24小时可显著缓解β淀粉样蛋白（Aβ1-42）诱导的大鼠海马细胞活力下降，增加活细胞数量并增强细胞活性[4]。10μM的Memantine hydrochloride处理人脐静脉内皮细胞（HUVECs）6小时能缓解氧糖剥夺/再灌注诱导的氧化应激，增加Nrf2和HO-1表达并提高细胞活力[5]。250μM的Memantine hydrochloride处理LNCaP细胞48小时可显著上调促凋亡蛋白Bax表达水平，并诱导细胞周期阻滞于G0/G1期[6]。
在体内，APP/PS1小鼠每日灌胃Memantine hydrochloride（20mg/kg；持续2个月）可改善空间学习能力并缓解记忆损伤[7]。克氏锥虫感染的BALB/c小鼠连续10天每日腹腔注射10mg/kg剂量的Memantine hydrochloride能减轻寄生虫血症，降低心脏寄生虫负荷和炎症浸润，并提高生存率[8]。
| Cell experiment [1]: | |
Cell lines | LNCaP cells |
Preparation Method | 3 × 103 LNCaP cells were inoculated into 100μL of culture medium in a 96-well plate and cultured for 24 hours. Different concentrations of Memantine hydrochloride (250, 500, 750, 1000, and 2000μM) were added to the culture medium, and the cells were further cultivated for 48h. MTT solution (5mg/mL PBS) was added to each well, and the culture plate was incubated at 37°C for 4 hours. The absorbance ratio was measured at 570nm on a microplate reader. |
Reaction Conditions | 250, 500, 750, 1000, and 2000μM; 48h |
Applications | Memantine hydrochloride treatment significantly inhibited cell proliferation of LNCaP cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | G93A transgenic mice |
Preparation Method | G93A transgenic mice were raised in a controlled environment (temperature 20-22℃, humidity 40-60%, light duration 07:00 to 19:00), with free access to food and water. The mice were randomly divided into a control group and a Memantine hydrochloride group (30mg/kg/day; p.o), with 10 mice in each group. The Memantine hydrochloride treatment was initiated at 75 days of age in mice, and the behavioral performance was evaluated twice a week using the rotating beam test, paw grip endurance (PaGE), and hindlimb extension reflex. The survival rate of the mice was recorded. The entire experiment lasted for 5 months. |
Dosage form | 30mg/kg/day for 5 months; p.o. |
Applications | Memantine hydrochloride treatment prolonged the survival period of transgenic mice and improved the motor ability of mice. |
References: | |
| Cas No. | 41100-52-1 | SDF | |
| 别名 | 盐酸美金刚; D-145 hydrochloride | ||
| 化学名 | 3,5-dimethyladamantan-1-amine;hydrochloride | ||
| Canonical SMILES | CC12CC3CC(C1)(CC(C3)(C2)N)C.Cl | ||
| 分子式 | C12H22ClN | 分子量 | 215.76 |
| 溶解度 | ≥ 12.6mg/mL in DMSO; ≥20 mg/mL in Water | 储存条件 | Store at RT |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.6348 mL | 23.1739 mL | 46.3478 mL |
| 5 mM | 0.927 mL | 4.6348 mL | 9.2696 mL |
| 10 mM | 0.4635 mL | 2.3174 mL | 4.6348 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet