| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Etimizol targets potassium channels and other purinergic signaling pathways. As a xanthine-related compound, it may modulate adenosine receptors and phosphodiesterase activity, similar to other xanthine derivatives such as caffeine and theophylline. Its nootropic and respiratory analeptic effects are likely mediated through modulation of neurotransmitter systems and improvement of cerebral circulation. The compound's ability to relieve amnesia in hypoxic conditions suggests that it may protect against hypoxia-induced neuronal damage.
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| ln Vitro |
In vitro studies on Etimizol are limited. As a xanthine-related compound, it may exhibit similar activities to other xanthine derivatives, including adenosine receptor antagonism, phosphodiesterase inhibition, and modulation of calcium homeostasis. The compound's respiratory analeptic effects suggest that it may stimulate respiratory centers in the brainstem. Its nootropic effects suggest that it may enhance cognitive function through modulation of neurotransmitter systems or improvement of cerebral blood flow. Detailed in vitro data are limited.
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| ln Vivo |
The amount of time that elapsed between the commencement of the research and the timidazole (3 mg/kg) injection varied in many series, ranging from 0.5 to 3 hours. Regardless of the biological type of reinforcement or the timing of delivery, etimizol (also known as ethymisole) does not improve learning in rats [1]. The mean residence times of etimizol (Ethymisole) in the circuit were 20.1 and 7.6 minutes, respectively, following the administration of etimizol (Ethymisole) at dosages of 10 or 1 mg/loop, with mean standard deviations of 3.1 and 0.8 [2]. Giant neurons in the isolated nervous system of horned beetles respond differently when 5--10 mM/L etimizol (Ethymisole) is applied extracellularly. These effects include a significant increase in action potential duration, a slowdown in the development of the decline phase, and a significant amplitude of trace hyperpolarization [3].
In vivo, Etimizol has been shown to relieve amnesia effectively in conditions with a hypoxic component, including hypobaric hypoxia, actinomycin D treatment, and mechanical injury of the brain. These findings suggest that Etimizol may have neuroprotective and cognitive-enhancing effects. The compound has been studied as a respiratory analeptic and nootropic agent. However, Etimizol is not widely used in current clinical practice and is primarily of research interest. |
| Enzyme Assay |
In vitro non-cell assays for Etimizol are limited. Standard assays for xanthine-related compounds include adenosine receptor binding assays using radiolabeled ligands, phosphodiesterase activity assays, and calcium flux measurements. These assays can be adapted to study Etimizol's mechanism of action, but specific published protocols for this compound are limited.
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| Cell Assay |
In vitro cell-based assays for Etimizol use neuronal cell lines or primary neurons to study its effects on neuronal survival, neurotransmitter release, and signaling pathways. Cells are treated with Etimizol under hypoxic conditions to evaluate its neuroprotective effects. Parameters assessed include cell viability, apoptosis markers, and neurotransmitter levels. However, specific published data for this compound are limited.
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| Animal Protocol |
In vivo animal studies for Etimizol employ rodent models of hypoxia-induced amnesia, such as hypobaric hypoxia, actinomycin D-induced amnesia, or mechanical brain injury models. The compound is administered orally or intraperitoneally, and cognitive function is assessed using behavioral tests such as the Morris water maze, passive avoidance, or novel object recognition tests. Histological examination of brain tissues may be performed to assess neuroprotection.
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| ADME/Pharmacokinetics |
Etimizol has a molecular weight of 210.23 g/mol and a molecular formula of C₉H₁₄N₄O₂. It is freely soluble in water at 391 g/L (25°C) and has a density of 1.26±0.1 g/cm³. The compound is also known as Ethymisole, Antiffine, and Ethylnorantifein. It is soluble in DMSO at 10 mM. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of Etimizol has not been comprehensively evaluated in published studies. As a xanthine-related compound, it may have a safety profile similar to other xanthine derivatives, which are generally well-tolerated at therapeutic doses. However, high doses may cause central nervous system stimulation, cardiovascular effects, and gastrointestinal disturbances. The compound is classified as a research reagent and is not intended for human therapeutic use.
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| References |
[1]. Borisova GIu. Effect of etimizol on instrumental learning in rats. Biull Eksp Biol Med. 1985 Jun;99(6):705-6.
[2]. Trnovec T, et al. Etimizol absorption from the small intestine in dogs: the dependence on dosage. Biull Eksp Biol Med. 1986 Dec;102(12):729-30. [3]. Vislobokov AI, et al. Elektrophysiological parameters of mollusk neurons under the influence of etimizol. Fiziol Zh SSSR Im I M Sechenova. 1975 Jun;61(6):917-24. |
| Additional Infomation |
drug associated with xanthine that is presumed to have nootropic effects.
Etimizol is a synthetic xanthine-related compound with respiratory analeptic and nootropic properties. It is also known as Ethymisole, Antiffine, and Ethylnorantifein. The compound relieves amnesia in conditions with a hypoxic component. It targets potassium channels and other purinergic signaling pathways. Not approved for clinical use; intended for research purposes only. |
| Molecular Formula |
C9H14N4O2
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|---|---|
| Molecular Weight |
210.23306
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| Exact Mass |
210.112
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| CAS # |
64-99-3
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| PubChem CID |
6168
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| Appearance |
White to off-white solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
563.4ºC at 760 mmHg
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| Flash Point |
294.5ºC
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| Index of Refraction |
1.586
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| LogP |
0.771
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
257
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=C(C(NC)=O)N(CC)C=N1)NC
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| InChi Key |
RYRFAMRQBZNEPX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H14N4O2/c1-4-13-5-12-6(8(14)10-2)7(13)9(15)11-3/h5H,4H2,1-3H3,(H,10,14)(H,11,15)
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| Chemical Name |
1-ethyl-4-N,5-N-dimethylimidazole-4,5-dicarboxamide
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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) |
Ethanol :≥ 33.33 mg/mL (~158.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.89 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (11.89 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (11.89 mM) (saturation unknown) in 10% EtOH + 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 | 4.7567 mL | 23.7835 mL | 47.5670 mL | |
| 5 mM | 0.9513 mL | 4.7567 mL | 9.5134 mL | |
| 10 mM | 0.4757 mL | 2.3783 mL | 4.7567 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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