| Targets |
Phenotropil's mechanism of action is not fully understood but is believed to involve modulation of neurotransmitter systems. It is a GABA receptor activator. As a nootropic, it is thought to enhance cognitive function by improving cerebral blood flow, increasing oxygen and glucose utilization in the brain, and modulating neurotransmitter levels, including dopamine and acetylcholine. Phenotropil is a phenyl analogue of piracetam and is significantly more potent.
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|---|---|
| ln Vitro |
In vitro, Phenotropil's activity has been studied in various assays. As a GABA receptor activator, it may modulate inhibitory neurotransmission. Its effects on dopamine reuptake have also been reported. However, specific in vitro data, such as IC50 or EC50 values, are not detailed in standard product descriptions. Phenotropil is a research compound used to study cognitive enhancement and neuroprotection.
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| ln Vivo |
In vivo, Phenotropil has been shown to have nootropic, anti-amnesic, antidepressant, anticonvulsant, antipsychotic, and anxiolytic effects in animal models. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam. Phenotropil is approved in some countries for the treatment of various neurological and psychiatric conditions. However, it is not approved in many countries and is primarily a research compound.
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| Enzyme Assay |
In vitro assays for Phenotropil are not well-defined, as its precise molecular targets have not been fully characterized. Its effects on GABA receptors can be studied using receptor binding assays. Dopamine reuptake inhibition can be assessed using synaptosomal uptake assays. However, specific protocols are not detailed in standard product descriptions. Phenotropil is a research compound.
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| Cell Assay |
In vitro cell-based assays for Phenotropil are used to study its effects on neuronal cells. Neuronal cultures are treated with Phenotropil, and the effects on cell viability, neurite outgrowth, and neurotransmitter release are assessed. The compound's neuroprotective effects can be studied by exposing cells to toxic stimuli. These assays confirm the compound's neuroactive properties.
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| Animal Protocol |
In vivo animal experiments for Phenotropil are conducted in animal models of cognitive impairment, depression, and anxiety. In a typical study, Phenotropil is administered to rodents, and its effects on learning and memory are assessed using behavioral tests such as the Morris water maze or the passive avoidance test. Antidepressant activity is assessed using the forced swim test or tail suspension test. These studies confirm the compound's nootropic and psychotropic effects.
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| ADME/Pharmacokinetics |
Phenotropil has a molecular weight of 218.256 g/mol and a molecular formula of C12H14N2O2. It has a CAS number of 77472-70-9. It is a white to off-white solid powder. It has a density of 1.2±0.1 g/cm3. It is soluble in DMSO at ≥ 100 mg/mL. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties have been characterized, and Phenotropil is orally active.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Phenotropil is not provided in standard product descriptions. As a compound that is used clinically in some countries, its safety profile has been evaluated. However, specific toxicity data, such as LD50 or organ toxicity, are not detailed. Phenotropil is generally considered to have a favorable safety profile, but it may have side effects such as insomnia, headache, and irritability. As with all research chemicals, standard laboratory safety precautions should be followed when handling Phenotropil.
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| References | |
| Additional Infomation |
Phenotropil (Phenylpiracetam, Carphedone) is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug and is 30 to 60 times more potent than piracetam. Phenotropil has anti-amnesic, antidepressant, anticonvulsant, antipsychotic, and anxiolytic effects. Its mechanism of action involves GABA receptor activation and modulation of neurotransmitter systems. Phenotropil is approved in some countries for the treatment of various neurological and psychiatric conditions. It is also used as a research compound.
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| Molecular Formula |
C12H14N2O2
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|---|---|
| Molecular Weight |
218.256
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| Exact Mass |
218.105
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| CAS # |
77472-70-9
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| Related CAS # |
(R)-Phenylpiracetam;949925-07-9
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| PubChem CID |
132441
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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 |
486.4±45.0 °C at 760 mmHg
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| Flash Point |
247.9±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.580
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| LogP |
0.16
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| Hydrogen Bond Donor Count |
1
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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 |
285
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LYONXVJRBWWGQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N2O2/c13-11(15)8-14-7-10(6-12(14)16)9-4-2-1-3-5-9/h1-5,10H,6-8H2,(H2,13,15)
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| Chemical Name |
2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide
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| Synonyms |
Carphedone FonturacetamCarphedon Karfedon Phenotropil Phenylpiracetam
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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 (~458.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.45 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 (11.45 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 (11.45 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 | 4.5817 mL | 22.9085 mL | 45.8169 mL | |
| 5 mM | 0.9163 mL | 4.5817 mL | 9.1634 mL | |
| 10 mM | 0.4582 mL | 2.2908 mL | 4.5817 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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