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| 1mg |
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| 5mg |
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| Targets |
The primary molecular target of (RS)-AMPA is the AMPA subtype of ionotropic glutamate receptors (AMPARs), which are ligand-gated cation channels that mediate fast excitatory neurotransmission. As a potent agonist, (RS)-AMPA binds to and activates these receptors, leading to the opening of the cation channel and influx of sodium and calcium ions, resulting in neuronal depolarization. Importantly, research has demonstrated that (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors, making it a selective tool for studying AMPA receptor function.
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| ln Vitro |
In vitro studies have demonstrated that (RS)-AMPA induces concentration-dependent depolarization in cultured rat spinal and brainstem neurons. At a concentration of 10⁻⁵ M, it produces minimal depolarization (3-7 mV), while at 10⁻⁴ M, depolarization magnitude varies from 4 to 33 mV, showing significant variability across different neurons. (RS)-AMPA also enhances the discharge rate of spontaneously firing neurons and can trigger brief bursts of action potentials in quiescent cells. The effects of (RS)-AMPA on cell survival are critically dependent on developmental timing—exposure to the agonist significantly reduces cell survival only when treatment is initiated after 5 days in vitro, while antagonist treatment starting on the day of plating has a stronger survival-reducing effect.
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| ln Vivo |
Specific in vivo pharmacodynamic data for (RS)-AMPA is limited in the available literature. As a prototypical AMPA receptor agonist, its primary applications are in in vitro neuronal preparations rather than in vivo studies. Research on brainstem cell development suggests that exposure to excitatory amino acid receptor agonists at critical stages of embryogenesis may alter central nervous system development. This finding indicates potential in vivo relevance for the compound's biological activity. The compound is strictly intended for laboratory research use only.
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| Enzyme Assay |
Binding assays for (RS)-AMPA are typically performed using radiolabeled [³H]AMPA. A standard protocol involves using eGFP-fused recombinant rat full-length GluA2 receptor expressed in HEK293T/17 cells. Membranes or cells expressing the target receptor are incubated with (RS)-[³H]AMPA at varying concentrations for a specified duration. Non-specific binding is determined in the presence of excess unlabeled competitor. Incubations are terminated by rapid filtration through glass fiber filters, followed by washing with ice-cold buffer. The radioactivity retained on the filters is measured by liquid scintillation counting. Data are analyzed using non-linear regression to determine binding affinity parameters (Kd and Bmax).
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| Cell Assay |
Cellular assays for (RS)-AMPA typically utilize primary neuronal cultures or neuronal cell lines expressing AMPA receptors. A representative protocol involves dissociating embryonic rat brainstem cells (embryonic day 14) and culturing them in appropriate medium. Cells are treated with (RS)-AMPA at concentrations ranging from 10⁻⁵ to 10⁻⁴ M for designated time periods (e.g., 3 days) at different developmental stages (e.g., starting on day 0 or after 5 days in vitro). Cell survival is assessed by counting gamma-enolase-positive neurons, while cell proliferation is evaluated using 5-bromo-2′-deoxyuridine staining. Electrophysiological studies can also be performed to measure depolarization effects and action potential firing rates using whole-cell patch-clamp recordings.
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| Animal Protocol |
A limited in vivo protocol has been described for larval assays. For example, (RS)-AMPA hydrobromide is dissolved in filtered sea water to a stock concentration of 7.5 mM and then diluted to a final concentration of 500 µM. Larvae are incubated with the drug for approximately 10 minutes before beginning assays. Behavioral responses are then recorded and analyzed. This protocol represents a rare in vivo application of the compound; most research applications are restricted to in vitro and ex vivo preparations.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic parameters for (RS)-AMPA, including absorption, distribution, half-life, clearance, and bioavailability, have not been reported in the available literature. As an experimental research tool compound rather than a therapeutic candidate, comprehensive ADME profiling has not been performed. However, its physicochemical properties have been characterized: the compound has a molecular weight of 186.17 g/mol, a calculated LogP value of -0.77 (indicating high hydrophilicity), and a polar surface area of 109.3 Ų. The compound is soluble in water up to 1.86-10 mM with gentle warming. The powder is stable when stored at room temperature.
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| Toxicity/Toxicokinetics |
(RS)-AMPA is classified as an experimental research compound and is strictly intended for laboratory research use only, not for human diagnostic or therapeutic applications. Its primary recognized biological activity—excitotoxicity mediated by excessive AMPA receptor activation—can lead to neuronal damage or death. In vitro studies on brainstem cells have demonstrated that exposure to AMPA receptor agonists at critical developmental stages can significantly reduce neuronal cell survival. No specific data on acute toxicity (LD50), chronic toxicity, genotoxicity, or reproductive toxicity is available in the provided references. Standard safety precautions for laboratory handling include working in a well-ventilated area, wearing appropriate personal protective equipment (gloves, lab coat, safety goggles), and avoiding inhalation, ingestion, or skin contact. The compound is understood to be not hazardous according to transportation regulations.
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| References |
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| Molecular Formula |
C7H11CLN2O4
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| Molecular Weight |
222.63
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| CAS # |
2922283-04-1
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| Related CAS # |
(S)-AMPA;83643-88-3;(RS)-AMPA;77521-29-0;(RS)-AMPA hydrobromide;171259-81-7
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=C(C(=O)NO1)CC(C(=O)O)N.Cl
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| Synonyms |
(±)-AMPA hydrochloride
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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 Note: (1). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~125 mg/mL (~561.47 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4918 mL | 22.4588 mL | 44.9176 mL | |
| 5 mM | 0.8984 mL | 4.4918 mL | 8.9835 mL | |
| 10 mM | 0.4492 mL | 2.2459 mL | 4.4918 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.
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