| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Aniracetam's mechanism of action involves multiple neurotransmitter systems. Its primary targets are glutamate receptors, particularly the AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor, where it acts as a positive allosteric modulator that slows receptor desensitization. Additionally, Aniracetam modulates metabotropic glutamate receptor (mGluR) function and enhances phospholipase C activation. Beyond the glutamatergic system, the drug also interacts with other receptors: it modulates nicotinic acetylcholine receptors in the cholinergic system and inhibits 5-HT2A receptors as well as dopamine D2 receptors. This multi-target mode of action collectively constitutes the molecular basis for its cognitive-enhancing, anxiolytic, and neuroprotective effects.
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| ln Vitro |
Aniracetam significantly enhances various concentrations of cisternic acid and counteracts cell death caused by glutamate, kainic acid, or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid. In primary cultures of cerebellar granule cells, ester and trans-1-aminocyclopentane-1,3-dicarboxylate also produce a neuroprotective response [4]. In cerebellar granule cell primary cultures, aniracetam improves phospholipase C's mGluR-coupled stimulation [4].
In vitro studies demonstrate that Aniracetam significantly modulates glutamate receptors. In the CA1 region of rat hippocampal slices, Aniracetam potentiates ionotropic quisqualate (iQA) responses. At Schaffer collateral-commissural synapses, the drug enhances excitatory postsynaptic potentials (EPSPs). In primary cultures of cerebellar granule cells, Aniracetam concentration-dependently counteracts glutamate-, kainate-, or AMPA-induced cell death and greatly facilitates neuroprotective responses achieved by different concentrations of quisqualate and trans-ACPD. Furthermore, in recombinant receptor studies, Aniracetam exhibits significant positive allosteric modulation of AMPA-induced currents at concentrations exceeding 1000 μM. |
| ln Vivo |
Aniracetam (1 mM; 30-75 min) potentiates iQA receptors and greatly increases native synaptic transmission in rats [1]. Aniracetam (10-100 mg/kg; oral; single dosage) protects CO2-induced learning impairment in rats [2]. Aniracetam (30-300 mg/kg; oral; single dosage) increases the percentage of rats demonstrating passive avoidance [2].
Aniracetam exhibits significant in vivo activity in various animal models. In rat hippocampal experiments, 1 mM Aniracetam significantly potentiates iQA receptor-mediated synaptic transmission within 30-75 minutes. In cognitive function studies, oral administration of 10-100 mg/kg Aniracetam prevents CO₂-induced impairment of acquisition in hypercapnia model rats, with most significant effects observed at 30 and 50 mg/kg. In a scopolamine-induced passive avoidance memory impairment model, Aniracetam at 50 and 100 mg/kg significantly increases the percentage of rats exhibiting passive avoidance behavior. In an ECS-induced amnesia mouse model, the anti-amnesic activity reaches 83.0% at a dosage of 100 mg/kg. In anxiety models, Aniracetam exerts anxiolytic effects through GABAergic mechanisms. |
| Enzyme Assay |
For Aniracetam, a positive allosteric modulator of the AMPA receptor, cell-free studies can utilize radioligand binding assays. A typical protocol is as follows: 1) Prepare synaptic membranes rich in AMPA receptors from rat brain tissue or use cell membranes expressing recombinant AMPA receptors; 2) Dissolve Aniracetam in DMSO to prepare a stock solution and dilute to serial concentrations with binding buffer (containing 50 mM Tris-HCl, pH 7.4); 3) Add the radiolabeled AMPA receptor ligand [³H]-AMPA (final concentration approximately 5-10 nM); 4) Incubate for 60-90 minutes at 4°C or room temperature; 5) Terminate the reaction by rapid vacuum filtration and wash the filters with ice-cold buffer; 6) Measure membrane-bound radioactivity using a liquid scintillation counter and calculate the specific binding inhibition rate at each concentration.
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| Cell Assay |
The in vitro cell assay protocol for Aniracetam is as follows: 1) Seed target neuronal cells (such as primary cerebellar granule cell cultures or SH-SY5Y cells) in multi-well plates and culture to appropriate density at 37°C with 5% CO₂; 2) Pre-treat cells with various concentrations of Aniracetam (generally ranging from 10-1000 μM); 3) Expose to injury conditions: such as glutamate (100-500 μM), kainate (30-100 μM), or AMPA (10-100 μM) to induce excitotoxicity; 4) Measure cell viability using MTT assay or LDH release assay; 5) Detect apoptosis rate using flow cytometry or TUNEL staining; 6) Detect changes in expression of apoptosis-related proteins such as caspase-3, Bcl-2, and Bax by Western blot.
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| Animal Protocol |
Animal/Disease Models: Pyramidal neurons from male Wistar rats [1]
Doses: 1 mM Route of Administration: 30-75 minutes Experimental Results: Enhanced iQA receptors present in the brain and produced significant facilitation of native synaptic transmission . Animal/Disease Models: Male rat (100-120 g; pure CO2 induces hypercapnia) [2] Doses: 10, 30, 50 and 100 mg/kg Route of Administration: Oral; single dose (60 days before hypercapnia) minutes) Experimental Results: CO2-induced acquisition impairment was Dramatically prevented at doses of 30 and 50 mg/kg. Animal/Disease Models: Male rats and male mice (100-120 g and 21-25 g; 0.5 mg/kg scopolamine-induced transient memory impairment of passive avoidance procedures) [2] Doses: 30, 50, 100 and 300 mg/kg , Route of Administration: po; single dose Experimental Results: 2 hrs (hrs (hours)) after 50 and 100 mg/kg scopolamine, the percentage of rats showing passive avoidance increased Dramatically. The in vivo animal assay protocol for Aniracetam is as follows: 1) Use adult male SD rats (100-120 g) or mice (21-25 g); 2) Establish cognitive impairment models: use scopolamine (0.5 mg/kg, intraperitoneal injection) to induce memory impairment, or use pure CO₂ to induce hypercapnia model; 3) Dosing regimen: administer Aniracetam orally by gavage, with common dose range of 10-300 mg/kg, typically as a single dose 30-60 minutes before behavioral testing; 4) Behavioral testing: use passive avoidance test (step-down test) to assess memory retention, or use Morris water maze to assess spatial learning and memory; 5) ECS-induced amnesia model: administer electroconvulsive shock (ECS) to induce amnesia and evaluate drug effects on memory recovery; 6) Euthanize animals after experiments and collect brain tissue for biochemical analysis or histopathological examination. |
| ADME/Pharmacokinetics |
Biological Half-Life
1-2.5 hours Aniracetam exhibits favorable pharmacokinetic characteristics in vivo. The drug is rapidly absorbed after oral administration with high oral bioavailability. Its elimination half-life is approximately 1-2.5 hours. Unlike water-soluble piracetam, Aniracetam is the only lipid-soluble member of the racetam family, which contributes to its good oral absorption properties. Aniracetam is primarily metabolized in the liver by carboxylesterases, particularly human recombinant CES1, with Km values ranging from 85,000-95,000 nM. The drug readily penetrates the blood-brain barrier to reach the central nervous system and exert its pharmacological effects. Its logD7.4 value is 0.93, indicating moderate lipophilicity. |
| Toxicity/Toxicokinetics |
2196 mouse LD50 intraperitoneal 1180 mg/kg SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE; BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD Yakuri to Chiryo. Pharmacology and Therapeutics., 14(Suppl
2196 rat LD50 oral 4500 mg/kg Psychopharmacology, 78(104), 1982 [PMID:6817363] 2196 rat LD50 subcutaneous >5 gm/kg Drugs in Japan, -(45), 1995 2196 mouse LD50 oral 3648 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD; GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS Yakuri to Chiryo. Pharmacology and Therapeutics., 14(Suppl 2196 mouse LD50 intravenous >100 mg/kg Medicamentos de Actualidad., 30(9), 1994 |
| References |
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| Additional Infomation |
Aniracetam belongs to the pyrrolidine-2-one and N-acylpyrrolidine classes. It is a compound with antidepressant properties and can be used as a psychoactive enhancer. Pharmacodynamics: Aniracetam possesses broad-spectrum anxiolytic properties, which may be mediated through interactions between the cholinergic, dopaminergic, and serotonergic systems.
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| Molecular Formula |
C12H13NO3
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| Molecular Weight |
219.2365
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| Exact Mass |
219.089
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| Elemental Analysis |
C, 65.74; H, 5.98; N, 6.39; O, 21.89
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| CAS # |
72432-10-1
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| PubChem CID |
2196
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
399.7±34.0 °C at 760 mmHg
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| Melting Point |
−58 °C(lit.)
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| Flash Point |
195.5±25.7 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
0.27
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
282
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)C(=O)N2CCCC2=O
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| InChi Key |
ZXNRTKGTQJPIJK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H13NO3/c1-16-10-6-4-9(5-7-10)12(15)13-8-2-3-11(13)14/h4-7H,2-3,8H2,1H3
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| Chemical Name |
1-(4-methoxybenzoyl)pyrrolidin-2-one
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| Synonyms |
aniracetam; 72432-10-1; Draganon; Sarpul; 1-(4-Methoxybenzoyl)-2-pyrrolidinone;
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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 |
| 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 : ≥ 100 mg/mL (~456.12 mM)
H2O : ~0.33 mg/mL (~1.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.40 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (11.40 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 25.0 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: ≥ 2.5 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5612 mL | 22.8061 mL | 45.6121 mL | |
| 5 mM | 0.9122 mL | 4.5612 mL | 9.1224 mL | |
| 10 mM | 0.4561 mL | 2.2806 mL | 4.5612 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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