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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.
(RS)-AMPA hydrochloride selectively targets and activates the AMPA subtype of ionotropic glutamate receptors (iGluRs). It does not interfere with the binding sites of kainic acid or NMDA receptors. As an agonist, it mimics the action of glutamate, the primary excitatory neurotransmitter in the central nervous system, leading to neuronal depolarization and the initiation of fast excitatory synaptic transmission. |
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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.
Specific in vitro activity data is not provided in the search results. However, as a potent and selective AMPA receptor agonist, (RS)-AMPA hydrochloride is known to induce a rapid and potent excitatory response in neuronal cultures by directly opening AMPA receptor cation channels. This influx of sodium ions leads to membrane depolarization, which is a fundamental step in synaptic transmission and is widely used to study neuronal excitability and synaptic function in cellular models. |
| 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.
(RS)-AMPA hydrochloride has been used in research on Parkinson's disease, indicating potential in vivo applications. Additionally, as an AMPA receptor agonist with potential antidepressant activity, it may be used in animal models to study glutamatergic signaling and behavior. While specific in vivo protocols are not detailed, the compound would typically be administered systemically to investigate its role in CNS-related diseases and to validate AMPA receptors as therapeutic targets. |
| 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).
The affinity and selectivity of (RS)-AMPA hydrochloride for AMPA receptors can be determined using a radioligand binding assay. Procedure: Membranes prepared from rat brain (e.g., cortex or hippocampus) are incubated with a fixed concentration of a selective AMPA receptor radioligand, such as [3H]AMPA or [3H](S)-AMPA, in the presence of varying concentrations of the test compound. After incubation at 4degC to prevent internalization, bound radioactivity is separated from free by rapid filtration through glass fiber filters. Non-specific binding is defined in the presence of a high concentration of an AMPA receptor antagonist (e.g., NBQX). |
| 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.
The functional activation of AMPA receptors can be assessed in primary neuronal cultures. Procedure: Primary rat cortical or hippocampal neurons are cultured for 14-21 days. The cells are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4-AM) and placed in a fluorescence microscope or plate reader. Varying concentrations of (RS)-AMPA hydrochloride (e.g., 0.1 - 100 microM) are added, and the change in fluorescence (excitation 494 nm, emission 516 nm) is recorded. An increase in fluorescence indicates an AMPA-mediated calcium influx, which is a direct measure of receptor activation. The EC50 value is calculated from the dose-response curve. |
| 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.
The effects of (RS)-AMPA hydrochloride can be studied in animal models of neurological diseases. Procedure: Male Sprague-Dawley rats (200-250 g) are anesthetized and implanted with a guide cannula for intracerebroventricular (ICV) injection. (RS)-AMPA hydrochloride is dissolved in artificial cerebrospinal fluid (aCSF) and injected via the cannula at a dose of 25 nmol/microL. Behavioral responses, such as seizure activity, are monitored. Alternatively, in a Parkinson's disease model, unilateral injection of (RS)-AMPA into the striatum can cause contralateral turning behavior, which is quantified to assess the functional integrity of the nigrostriatal pathway. |
| 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.
Specific pharmacokinetic data for (RS)-AMPA hydrochloride is not provided in the search results. As a small, polar molecule (MW 222.63), it is expected to have a limited ability to cross the blood-brain barrier (BBB). Following systemic administration, concentrations in the central nervous system are likely low, which is why it is often administered directly into the brain (e.g., via intracerebroventricular injection) in pharmacological studies. |
| 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.
Specific toxicology data for (RS)-AMPA hydrochloride is not provided. As a potent excitatory amino acid agonist, excessive activation of AMPA receptors can lead to excitotoxicity, a process where neurons are damaged and killed by excessive stimulation by neurotransmitters. This is a known mechanism of neuronal cell death in stroke, epilepsy, and traumatic brain injury. Therefore, careful handling is required, and standard safety precautions for research chemicals should be followed. |
| References |
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| Additional Infomation |
(RS)-AMPA hydrochloride is a research compound that is not an approved drug. It is widely used in neuroscience to study the structure and function of AMPA receptors, which are key mediators of fast synaptic transmission and plasticity. The discovery of AMPA receptors and their role in synaptic plasticity has been fundamental to the field of learning and memory. As a research tool, (RS)-AMPA hydrochloride is essential for studying the pathophysiology of various CNS disorders, including Parkinson's disease, depression, and epilepsy, and for the development of new therapeutics that target glutamatergic signaling.
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| Molecular Formula |
C7H11CLN2O4
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|---|---|
| Molecular Weight |
222.63
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| Exact Mass |
222.041
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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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| PubChem CID |
168431732
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
284
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=O)NO1)CC(C(=O)O)N.Cl
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| InChi Key |
CKVBWVWGMKTZAG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H10N2O4.ClH/c1-3-4(6(10)9-13-3)2-5(8)7(11)12;/h5H,2,8H2,1H3,(H,9,10)(H,11,12);1H
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| Chemical Name |
2-amino-3-(5-methyl-3-oxo-1,2-oxazol-4-yl)propanoic acid;hydrochloride
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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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