| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Nebracetam targets the M1-muscarinic acetylcholine receptor, a G protein-coupled receptor that is expressed in the central nervous system and plays a key role in learning and memory. Activation of M1 receptors leads to the activation of phospholipase C, production of inositol trisphosphate (IP3), and release of calcium from intracellular stores. Nebracetam induces a rise in intracellular calcium concentration with an EC50 of 1.59 mM. By activating M1 receptors, nebracetam modulates neuronal excitability and synaptic plasticity, which may underlie its cognitive-enhancing effects.
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| ln Vitro |
In vitro, nebracetam induces a rise in intracellular calcium concentration in cultured neurons with an EC50 of 1.59 mM. The compound's activity at the M1-muscarinic receptor is assessed by measuring calcium mobilization in cells expressing the receptor. Nebracetam's cognitive-enhancing and neuroprotective properties have been demonstrated in various in vitro models. The compound's ability to modulate intracellular calcium signaling may contribute to its effects on neuronal function.
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| ln Vivo |
Nebracetam (10 mg/kg, oral) includes not only cholinergic pathways, but also lymphatic and hippocampus noradrenergic mechanisms [2].
In vivo, nebracetam has been investigated for its cognitive-enhancing effects in animal models. The compound has been evaluated in models of learning and memory, including passive avoidance, Morris water maze, and novel object recognition tests. Nebracetam has shown efficacy in improving cognitive function in animal models of cognitive impairment. The compound's neuroprotective properties have also been investigated in models of neurodegeneration. |
| Enzyme Assay |
Nebracetam's activity at the M1-muscarinic receptor is assessed using cell-based functional assays. Cells expressing the M1 receptor are treated with varying concentrations of nebracetam; intracellular calcium concentration is measured using fluorescent calcium indicators (e.g., Fura-2, Fluo-4); EC50 values are calculated from dose-response curves. Selectivity for M1 over other muscarinic receptor subtypes is assessed by comparing activity at M1, M2, M3, M4, and M5 receptors. These assays provide quantitative information on the potency and selectivity of nebracetam.
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| Cell Assay |
Nebracetam is tested on cultured neurons and other cell types. Cells are treated with varying concentrations of nebracetam; intracellular calcium concentration is measured using fluorescent calcium indicators; neuronal viability is assessed by MTT or LDH assays following exposure to neurotoxic insults; synaptic plasticity is assessed by measuring dendritic spine density or electrophysiological recordings. These cell-based assays demonstrate the mechanism of action and neuroprotective activity of nebracetam.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat, weighing 200-250 grams [2].
Doses: 10, 20 mg/kg. Doses: PO (single dose). Experimental Results: Ability to correct scopolamine-induced disruption of spatial cognition. Nebracetam has been evaluated in animal models of cognitive impairment and neurodegeneration. In these models, nebracetam is administered orally or intraperitoneally; cognitive function is assessed using behavioral tests; neuronal survival and synaptic plasticity are assessed by histological and biochemical analyses. These in vivo studies provide evidence for the cognitive-enhancing and neuroprotective effects of nebracetam. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of nebracetam have been conducted in preclinical species. The compound's absorption, distribution, metabolism, and excretion have been characterized. Nebracetam crosses the blood-brain barrier, consistent with its central nervous system activity.
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| Toxicity/Toxicokinetics |
The toxicity profile of nebracetam is consistent with that of other racetam compounds. Racetams are generally well-tolerated at therapeutic doses, with common adverse effects including headache, nausea, and gastrointestinal disturbances. Comprehensive toxicological studies are needed to fully characterize the safety profile of nebracetam.
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| References | |
| Additional Infomation |
Nebracetam hydrochloride is a nootropic M1-muscarinic agonist that induces a rise in intracellular calcium concentration with an EC50 of 1.59 mM. The compound is being investigated for its potential cognitive-enhancing and neuroprotective properties. Nebracetam belongs to the racetam family of nootropic agents, which includes piracetam, aniracetam, and oxiracetam. The compound is used in research for studying cognitive enhancement, neuroprotection, and the role of muscarinic receptors in neuronal function. Nebracetam is not approved as a therapeutic agent and is used for research purposes only.
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| Molecular Formula |
C12H17CLN2O
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|---|---|
| Molecular Weight |
240.729182004929
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| Exact Mass |
240.102
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| CAS # |
1177279-49-0
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| PubChem CID |
71757437
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
224
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C1CC(CN)CN1CC1C=CC=CC=1
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| InChi Key |
KUXPUFAJKYNPMO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H16N2O.ClH/c13-7-11-6-12(15)14(9-11)8-10-4-2-1-3-5-10;/h1-5,11H,6-9,13H2;1H
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| Chemical Name |
4-(aminomethyl)-1-benzylpyrrolidin-2-one;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: 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 : ~100 mg/mL (~415.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.39 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 (10.39 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 (10.39 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 | 4.1540 mL | 20.7702 mL | 41.5403 mL | |
| 5 mM | 0.8308 mL | 4.1540 mL | 8.3081 mL | |
| 10 mM | 0.4154 mL | 2.0770 mL | 4.1540 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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