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| Other Sizes |
| Targets |
Etilefrine hydrochloride targets α1 and β1 adrenergic receptors. It acts as an adrenergic agonist, selectively binding to and activating α1-adrenergic receptors in arterioles and veins. Activation of α1 receptors causes smooth muscle contraction, leading to vasoconstriction and increased peripheral resistance. β1 receptor activation enhances myocardial contractility and elevates heart rate.
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| ln Vitro |
In vitro, Etilefrine hydrochloride acts as an adrenergic agonist, stimulating α1 and β1 adrenergic receptors. It activates AMPK and induces vasoconstriction in isolated vascular preparations. The compound's activity at α1 receptors leads to contraction of vascular smooth muscle. Specific IC50 or EC50 values for receptor activation are not extensively documented in publicly available literature.
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| ln Vivo |
In vivo, Etilefrine hydrochloride is used as a vasoconstrictor for the treatment of orthostatic hypotension. It increases blood pressure by stimulating α1 receptors, leading to vasoconstriction and decreased venous pooling. β1 receptor activation enhances cardiac contractility and output. The compound has been studied for the treatment of levodopa-induced orthostatic hypotension.
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| Enzyme Assay |
The in vitro receptor binding assay for Etilefrine hydrochloride involves measuring its affinity for α1 and β1 adrenergic receptors. Radiolabeled ligand binding assays are performed using membrane preparations from cells expressing α1 or β1 receptors. Varying concentrations of Etilefrine hydrochloride are incubated with the receptor preparation, and binding affinity (IC50 or Ki) is determined. The compound acts as an agonist at α1 and β1 receptors.
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| Cell Assay |
In vitro cellular assays for Etilefrine hydrochloride involve treating cultured vascular smooth muscle cells or cardiomyocytes with varying concentrations of the compound. Receptor activation is assessed by measuring intracellular calcium mobilization or cAMP levels. Smooth muscle contraction is measured using isolated vessel preparations. AMPK activation is assessed by Western blotting for phosphorylated AMPK.
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| Animal Protocol |
In vivo animal experiments for Etilefrine hydrochloride typically use rodent models of orthostatic hypotension or shock. The compound is administered via intravenous or oral routes at various doses. Blood pressure and heart rate are measured using tail-cuff or telemetry methods. Vasoconstriction is assessed by measuring peripheral resistance. The compound's pressor effects are compared to reference vasoconstrictors.
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| ADME/Pharmacokinetics |
Etilefrine hydrochloride has a half-life of approximately 2-2.5 hours. It is subject to significant first-pass metabolism, leading to a bioavailability of about 30-40%. The compound has a molecular weight of 217.69 (C10H15NO2·HCl). Etilefrine hydrochloride is metabolized in the liver and excreted via the kidneys. A washout period of at least 12.5 hours is recommended for pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Etilefrine hydrochloride is a clinically used vasoconstrictor with an established safety profile. Common adverse effects may include hypertension, tachycardia, palpitations, and headache. The compound is contraindicated in patients with severe hypertension, pheochromocytoma, or tachyarrhythmias. Regular monitoring of blood pressure and heart rate is required during treatment. Complete toxicology data are available from the drug's clinical use.
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| References |
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| Additional Infomation |
Etilefrine hydrochloride (TN) belongs to the phenolic compound class. It is a phenylephrine-type β-1-adrenergic and α-adrenergic agonist, used as a cardiotonic and antihypertensive agent.
Etilefrine hydrochloride (CAS#: 943-17-9) is the hydrochloride salt of etilefrine, a sympathetic nerve agonist and AMPK activator that selectively targets α1 and β1 adrenergic receptors. It is used as a vasoconstrictor for the treatment of orthostatic hypotension. Etilefrine hydrochloride stimulates α1 receptors to cause vasoconstriction and increased peripheral resistance, and activates β1 receptors to enhance cardiac contractility. The hydrochloride salt form enhances aqueous solubility for pharmaceutical formulations. |
| Molecular Formula |
C10H15NO2.HCL
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|---|---|
| Molecular Weight |
217.69254
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| Exact Mass |
217.086
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| CAS # |
943-17-9
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| Related CAS # |
Etilefrine;709-55-7
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| PubChem CID |
164652
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| Appearance |
White to off-white solid powder
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| Density |
1.127g/cm3
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| Boiling Point |
351.7ºC at 760 mmHg
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| Melting Point |
122ºC
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| Flash Point |
155.5ºC
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| LogP |
2.228
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
141
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KTNROWWHOBZQGK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15NO2.ClH/c1-2-11-7-10(13)8-4-3-5-9(12)6-8;/h3-6,10-13H,2,7H2,1H3;1H
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| Chemical Name |
3-[2-(ethylamino)-1-hydroxyethyl]phenol;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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.5937 mL | 22.9684 mL | 45.9369 mL | |
| 5 mM | 0.9187 mL | 4.5937 mL | 9.1874 mL | |
| 10 mM | 0.4594 mL | 2.2968 mL | 4.5937 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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