| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
NMDA (N-Methyl-D-aspartic acid; LC488A; LC488 A; LC488-A; LC 488A; LC-488A) is an aspartic acid analog with an N-methyl substituent and D-configuration and a glutamate-like excitatory chemical substance. It acts as a potent and specific agonist for NMDA receptor mimicking the action of glutamate, which is a neurotransmitter acting at NMDA receptors.
| Targets |
N-methyl-D-aspartic acid (NMDA) receptor [1]
N-methyl-D-aspartic acid (NMDA) receptor [2] N-methyl-D-aspartic acid (NMDA) receptor [3] |
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| ln Vitro |
Regardless of the incubation temperature, NMDA dramatically increases adrenal binding in a concentration-dependent manner [2].
In rat adrenal membrane preparations, NMDA (N-Methyl-D-aspartic acid) enhanced the binding of [3H]glutamate in a concentration-dependent manner. The enhancement was significant at concentrations ≥100 μM, with maximal binding increase observed at 1 mM [2] In cultured dorsal root ganglion (DRG) neurons from rats with neuropathic pain, activation of NMDA (N-Methyl-D-aspartic acid) receptor increased neuronal excitability, as indicated by enhanced action potential firing and elevated intracellular calcium concentration. This effect was blocked by NMDA receptor antagonists [3] |
| ln Vivo |
NMDA (0.2 nM) had a substantial effect on MF, IF, IL, and EL, reducing installation and insertion frequency while shortening insertion and ejaculation times. During the 30-minute mating test, NMDA and AP-5 significantly increased and decreased ejaculation behavior, respectively. Bilateral microinjection of NMDA into the PVN significantly raised baseline LSNA, with the greatest rise happening within 5 minutes [1].
In male rats, microinjection of NMDA (N-Methyl-D-aspartic acid) into the paraventricular nucleus (PVN) of the hypothalamus induced ejaculatory responses in a dose-dependent manner. The effective dose range was 0.1-1 μg/0.5 μL, and the response was abolished by pretreatment with the NMDA receptor antagonist AP5. The ejaculatory effect was mediated via sympathetic outflow, as demonstrated by reduced responses after sympathetic nerve blockade [1] In a rat model of neuropathic pain induced by sciatic nerve ligation, decreased expression of growth and differentiation factor 10 (GDF10) led to activation of NMDA (N-Methyl-D-aspartic acid) receptor in the spinal cord. This activation contributed to mechanical allodynia and thermal hyperalgesia, which were reversed by NMDA receptor inhibition [3] |
| Enzyme Assay |
[3H]glutamate binding assay in rat adrenal membranes: Prepare crude membrane fractions from rat adrenal glands by homogenization and differential centrifugation. Suspend membrane pellets in incubation buffer and incubate with [3H]glutamate (fixed concentration) and various concentrations of NMDA (N-Methyl-D-aspartic acid) at 25°C for 60 minutes. Terminate the reaction by rapid filtration through glass fiber filters pre-soaked in buffer. Wash filters thoroughly with ice-cold buffer to remove unbound ligand, then measure radioactivity using a liquid scintillation counter. Calculate specific binding as total binding minus non-specific binding (in the presence of excess unlabeled glutamate) [2]
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| Cell Assay |
Dorsal root ganglion (DRG) neuron culture and excitability assay: Isolate DRG from adult rats, dissociate into single neurons by enzymatic digestion and mechanical trituration, and seed onto poly-L-lysine-coated coverslips. Culture neurons in neurobasal medium supplemented with growth factors for 3-5 days. Treat neurons with NMDA (N-Methyl-D-aspartic acid) (10-100 μM) and record action potentials using patch-clamp technique in current-clamp mode. Measure intracellular calcium concentration using a calcium-sensitive fluorescent dye, with fluorescence intensity recorded by confocal microscopy [3]
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| Animal Protocol |
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. 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] |
| References |
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| Additional Infomation |
N-methyl-D-aspartic acid is an aspartic acid derivative with an N-methyl substituent and a D-configuration. It is a neurotransmitter. It is a D-α-amino acid, a D-aspartic acid derivative, an aminodicarboxylic acid, and a secondary amino compound.
This amino acid, its D-isomer, is a characteristic agonist of the NMDA receptor subtype (RECEPTORS, NMDA). NMDA (N-methyl-D-aspartic acid) is an endogenous amino acid and a selective agonist of the NMDA receptor (an ionotropic glutamate receptor subtype)[1]. It requires the co-binding of glutamate and glycine to activate the NMDA receptor, resulting in the opening of receptor-associated ion channels, the influx of calcium and sodium ions, and subsequently, neuronal excitation[2]. In the paraventricular nucleus (PVN) of the hypothalamus, NMDA (N-methyl-D-aspartate)-induced NMDA receptor activation regulates ejaculation through the following pathways: The sympathetic nervous system provides important clues for understanding the central control of male sexual behavior [1] In neuropathic pain, downregulation of GDF10 eliminates its inhibitory effect on NMDA (N-methyl-D-aspartate) receptors, leading to receptor overactivation and spinal cord sensitization, thereby exacerbating pain hypersensitivity [3] |
| Molecular Formula |
C5H9NO4
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| Molecular Weight |
147.13
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| Exact Mass |
147.053
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| CAS # |
6384-92-5
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| Related CAS # |
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| PubChem CID |
22880
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
258.2±30.0 °C at 760 mmHg
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| Melting Point |
187-192 °C
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| Flash Point |
110.0±24.6 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.494
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| LogP |
-0.44
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
10
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| Complexity |
145
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN[C@H](CC(=O)O)C(=O)O
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| InChi Key |
HOKKHZGPKSLGJE-GSVOUGTGSA-N
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| InChi Code |
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
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| Chemical Name |
(2R)-2-(methylamino)butanedioic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (6.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 36.67 mg/mL (249.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.7967 mL | 33.9836 mL | 67.9671 mL | |
| 5 mM | 1.3593 mL | 6.7967 mL | 13.5934 mL | |
| 10 mM | 0.6797 mL | 3.3984 mL | 6.7967 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06183788 | Recruiting | Behavioral: Remote cognitive rehabilitation program |
Anti-NMDA Receptor Encephalitis | Fundacion Clinic per a la Recerca Biomédica | January 16, 2023 | Not Applicable |
| NCT05977023 | Recruiting | Drug: NMDAE Drug: Placebo Cap |
Bipolar I Disorder | China Medical University Hospital | October 4, 2023 | Phase 2 |
| NCT05136755 | Recruiting | Drug: NMDAE Drug: Placebo Cap |
Major Depressive Disorder | China Medical University Hospital | January 25, 2022 | Phase 2 |
| NCT04745143 | Recruiting | Drug: NMDAE Drug: Placebo Cap |
Schizophrenia | China Medical University Hospital | January 1, 2018 | Phase 2 |
| NCT02950233 | Terminated | Drug: NMDA active Drug: Steroid active Drug: NMDA placebo Drug: Steroid placebo |
Pain, Postoperative | Population Health Research Institute | May 4, 2017 | Phase 3 |
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