NMDA (N-Methyl-D-aspartic acid)   中文名称: N-甲基-D-天冬氨酸

N-methyl-D-aspartic acid (NMDA) receptor [1]
N-methyl-D-aspartic acid (NMDA) receptor [2]
N-methyl-D-aspartic acid (NMDA) receptor [3]

无论孵育温度如何，NMDA 都会以浓度依赖性方式显着增加肾上腺结合 [2]。

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在大鼠肾上腺膜制剂中，NMDA（N-甲基-D-天冬氨酸）以浓度依赖方式增强[3H]谷氨酸的结合。浓度≥100 μM时增强效果显著，在1 mM时观察到最大结合增加[2]
在神经病理性疼痛大鼠的背根神经节（DRG）神经元培养物中，NMDA（N-甲基-D-天冬氨酸）受体激活可增加神经元兴奋性，表现为动作电位发放增强和细胞内钙浓度升高，该效应可被NMDA受体拮抗剂阻断[3]

NMDA (0.2 nM) 对 MF、IF、IL 和 EL 有显着影响，减少安装和插入频率，同时缩短插入和射精时间。在 30 分钟的交配测试中，NMDA 和 AP-5 分别显着增加和减少射精行为。将 NMDA 双边显微注射到 PVN 中可显着提高基线 LSNA，最大升幅发生在 5 分钟内 [1]。

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在雄性大鼠中，向丘脑下部室旁核（PVN）微量注射NMDA（N-甲基-D-天冬氨酸）可剂量依赖诱导射精反应，有效剂量范围为0.1-1 μg/0.5 μL。用NMDA受体拮抗剂AP5预处理可消除该反应，且交感神经阻滞后续发反应降低，表明射精效应通过交感神经传出介导[1]
在坐骨神经结扎诱导的大鼠神经病理性疼痛模型中，生长分化因子10（GDF10）表达降低导致脊髓中NMDA（N-甲基-D-天冬氨酸）受体激活，该激活可引发机械痛觉过敏和热痛觉过敏，NMDA受体抑制可逆转这些症状[3]

大鼠肾上腺膜[3H]谷氨酸结合实验：通过匀浆和差速离心从大鼠肾上腺制备粗膜组分，将膜沉淀悬浮于孵育缓冲液中，与固定浓度的[3H]谷氨酸和不同浓度的NMDA（N-甲基-D-天冬氨酸）在25°C孵育60分钟。通过预浸泡在缓冲液中的玻璃纤维滤膜快速过滤终止反应，用冰浴缓冲液彻底洗涤滤膜以去除未结合配体，随后通过液体闪烁计数器测定放射性强度。特异性结合计算为总结合减去非特异性结合（在过量未标记谷氨酸存在下）[2]

背根神经节（DRG）神经元培养与兴奋性检测：从成年大鼠分离DRG，通过酶解和机械研磨分散为单个神经元，接种到多聚-L-赖氨酸包被的盖玻片上。在添加生长因子的神经基底培养基中培养神经元3-5天，用NMDA（N-甲基-D-天冬氨酸）（10-100 μM）处理神经元，采用膜片钳技术在电流钳模式下记录动作电位。使用钙敏感荧光染料检测细胞内钙浓度，通过共聚焦显微镜记录荧光强度[3]

0.20 nmol in 100 nL saline
Rats: Thirty male rats are paired with different receptive females for a total of three times (once every 3 days) a week prior to the experiment, only the males that ejaculated at least three times during this period are included. After selecting the male rats with normal ejaculatory ability. Saline (100 nL), NMDA (0.20 nmol in 100 nL saline), and AP-5 (10.0 nmol in 100 nL saline) are adminitration into the bilateral PVN of each male rat in random order. After 5 min, the behavioral testing is performed and recorded as described above. Copulatory behaviors occur once a week and the entire experiment lasted 4 weeks.

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PVN microinjection and ejaculatory response assay in rats: Adult male rats are anesthetized and placed in a stereotaxic frame. A guide cannula is implanted targeting the PVN based on stereotaxic coordinates. After a 7-day recovery period, NMDA (N-Methyl-D-aspartic acid) is dissolved in artificial cerebrospinal fluid (aCSF) and injected into the PVN at doses of 0.1, 0.5, or 1 μg/0.5 μL via an injection cannula connected to a microsyringe. Ejaculatory behavior (number of ejaculations, latency) is recorded for 30 minutes after injection. For antagonist studies, AP5 is injected 10 minutes before NMDA administration [1]
Sciatic nerve ligation-induced neuropathic pain model in rats: Adult rats are anesthetized, and the left sciatic nerve is exposed and loosely ligated with chromic gut sutures. Sham-operated rats undergo nerve exposure without ligation. Two weeks after surgery, mechanical allodynia (paw withdrawal threshold to von Frey filaments) and thermal hyperalgesia (paw withdrawal latency to radiant heat) are assessed. To evaluate the role of NMDA receptor, NMDA (N-Methyl-D-aspartic acid) receptor antagonists are administered intraperitoneally, and behavioral tests are repeated 30 minutes later [3]

[1]. Centrally mediated ejaculatory response via sympathetic outflow in rats: role of N-methyl-D-aspartic acid receptors in paraventricular nucleus. Andrology. 2016 Nov 16.

[2]. Enhancement of [3H]glutamate binding by N-methyl-D-aspartic acid in rat adrenal. Brain Res. 1987 Mar 17;406(1-2):24-31.

[3]. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-methyl-D-aspartate receptor activation. Neuroreport. 2017 May 24;28(8):444-450.

N-methyl-D-aspartic acid is an aspartic acid derivative having an N-methyl substituent and D-configuration. It has a role as a neurotransmitter agent. It is a D-alpha-amino acid, a D-aspartic acid derivative, an amino dicarboxylic acid and a secondary amino compound.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).

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NMDA (N-Methyl-D-aspartic acid) is an endogenous amino acid and a selective agonist of the NMDA receptor, a subtype of ionotropic glutamate receptors [1]
Its activation of NMDA receptor requires co-binding of glutamate and glycine, leading to opening of the receptor-associated ion channel, influx of calcium and sodium ions, and subsequent neuronal excitation [2]
In the hypothalamic PVN, NMDA (N-Methyl-D-aspartic acid)-induced NMDA receptor activation regulates ejaculatory function via the sympathetic nervous system, providing insights into the central control of male sexual behavior [1]
In neuropathic pain, downregulation of GDF10 removes its inhibitory effect on NMDA (N-Methyl-D-aspartic acid) receptor, leading to excessive receptor activation and spinal sensitization, which contributes to pain hypersensitivity [3]

C5H9NO4

147.13

147.053

6384-92-5

22880

White to off-white solid powder

1.3±0.1 g/cm3

258.2±30.0 °C at 760 mmHg

187-192 °C

110.0±24.6 °C

0.0±1.1 mmHg at 25°C

1.494

-0.44

86.63

3

5

4

10

145

1

CN[C@H](CC(=O)O)C(=O)O

HOKKHZGPKSLGJE-GSVOUGTGSA-N

InChI=1S/C5H9NO4/c1-6-3(5(9)10)2-4(7)8/h3,6H,2H2,1H3,(H,7,8)(H,9,10)/t3-/m1/s1

(2R)-2-(methylamino)butanedioic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 1 mg/mL (6.80 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 10.0 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 1 mg/mL (6.80 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 10.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 1 mg/mL (6.80 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 10.0 mg/mL 澄清 DMSO 储备液加入900 μL 玉米油中，混合均匀。

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配方 4 中的溶解度: 36.67 mg/mL (249.24 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。