| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Ethylnorepinephrine hydrochloride targets adrenergic receptors (alpha- and beta-adrenergic receptors) in the sympathetic nervous system. As a sympathomimetic agent structurally related to norepinephrine, it acts as an agonist at these receptors. Specifically, it has bronchodilator properties, indicating activity at beta2-adrenergic receptors in the lungs. It may also have alpha-adrenergic agonist activity, leading to vasoconstriction and increased blood pressure. The ethyl substitution modulates its receptor selectivity and duration of action compared to norepinephrine.
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| ln Vitro |
As a sympathomimetic, Ethylnorepinephrine hydrochloride would be expected to elicit functional responses in adrenergic receptor-expressing cells, such as increased cAMP production (via beta-adrenoceptors) and calcium mobilization (via alpha-adrenoceptors). The specific IC50 or EC50 values are not provided. The compound has been used as a bronchodilator, indicating that it relaxes bronchial smooth muscle at therapeutic concentrations. The hydrochloride salt enhances aqueous solubility for parenteral administration.
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| ln Vivo |
Ethylnorepinephrine hydrochloride has been used clinically as a bronchodilator under the trade name Bronkephrine. In animal models, administration would be expected to cause bronchodilation, increased heart rate, and elevation of blood pressure due to activation of beta1- and alpha-adrenergic receptors, respectively. Specific in vivo efficacy data is not provided, but the compound has been used to treat asthma and bronchospasm.
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| Enzyme Assay |
Not applicable. Ethylnorepinephrine hydrochloride is a small molecule agonist, not used in cell-free binding assays for routine characterization. However, its affinity for adrenergic receptors can be determined by radioligand binding. Procedure: Membranes from HEK293 cells expressing human beta2-adrenergic receptors (20 ug/well) are incubated with 0.1 nM [3H]-dihydroalprenolol (DHA) and varying concentrations of Ethylnorepinephrine hydrochloride (0.1-1000 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 10 mM MgCl2, 2 mM EDTA) for 60 minutes at 25degC. Non-specific binding is determined with 10 uM propranolol. Bound radioligand is separated by filtration through GF/B filters and counted. The Ki is calculated from the IC50.
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| Cell Assay |
Functional adrenergic receptor activation can be assessed in cells expressing beta2-adrenergic receptors using a cAMP accumulation assay. Procedure: CHO-K1 cells stably expressing the human beta2-adrenergic receptor are seeded in 384-well plates (20,000 cells/well). Cells are pre-incubated with 1 mM IBMX (phosphodiesterase inhibitor) for 10 minutes, then treated with varying concentrations of Ethylnorepinephrine hydrochloride (0.1-1000 nM) for 30 minutes at 37degC. The reaction is stopped with lysis buffer, and intracellular cAMP levels are measured using a homogeneous time-resolved fluorescence (HTRF) cAMP detection kit. The EC50 is calculated from the dose-response curve.
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| Animal Protocol |
The in vivo efficacy as a bronchodilator can be evaluated in a guinea pig model of histamine-induced bronchospasm. Procedure: Male Hartley guinea pigs (300-400 g, n=8 per group) are anesthetized. The trachea is cannulated and connected to a ventilator to measure pulmonary resistance. Bronchospasm is induced by an intravenous injection of histamine (30 ug/kg). Ethylnorepinephrine hydrochloride is dissolved in saline and administered intravenously at doses of 0.1, 0.5, and 1 mg/kg, 5 minutes before histamine challenge. The positive control group receives isoproterenol (1 mg/kg). The reduction in histamine-induced increase in pulmonary resistance is measured. An ED50 for bronchodilation is calculated.
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| ADME/Pharmacokinetics |
Specific PK data for Ethylnorepinephrine hydrochloride is not provided. As a catecholamine, it is rapidly metabolized by catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO), resulting in a short plasma half-life (minutes). It is poorly absorbed orally and is administered by inhalation or injection. The compound is stored as a powder at -20degC (3 years) or 4degC (2 years).
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| Toxicity/Toxicokinetics |
Specific toxicology data for Ethylnorepinephrine hydrochloride is not provided. As a sympathomimetic agent, potential adverse effects include tachycardia, hypertension, cardiac arrhythmias, anxiety, and tremors. Overdose can lead to severe hypertension and cardiac events. Standard safety precautions for handling catecholamines should be followed.
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| Additional Infomation |
See also: Ethylnorepinephrine (has active moiety).
Ethylnorepinephrine hydrochloride is a sympathomimetic amine and bronchodilator structurally related to norepinephrine. It was marketed under the trade name Bronkephrine for the treatment of asthma and bronchospasm. It acts as an agonist at beta2-adrenergic receptors in the lungs, causing bronchodilation, but also has alpha- and beta1-adrenergic agonist activity, which can cause cardiovascular effects. This product is a research chemical and is not intended for clinical use. It is used for research on adrenergic receptor pharmacology and as a reference standard for pharmaceutical analysis. |
| Molecular Formula |
C10H16CLNO3
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|---|---|
| Molecular Weight |
233.69
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| Exact Mass |
233.082
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| CAS # |
3198-07-0
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| PubChem CID |
18900
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| Appearance |
Solid Powder
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| Melting Point |
199-200℃ (dec)
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| LogP |
2.371
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
177
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC(C(C1C=CC(O)=C(O)C=1)O)N
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| InChi Key |
NZDMRJGAFPUTMZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15NO3.ClH/c1-2-7(11)10(14)6-3-4-8(12)9(13)5-6;/h3-5,7,10,12-14H,2,11H2,1H3;1H
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| Chemical Name |
4-(2-amino-1-hydroxybutyl)benzene-1,2-diol;hydrochloride
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| Synonyms |
Etanor hydrochloride; Butanephrine 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 |
| 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 | 4.2792 mL | 21.3959 mL | 42.7917 mL | |
| 5 mM | 0.8558 mL | 4.2792 mL | 8.5583 mL | |
| 10 mM | 0.4279 mL | 2.1396 mL | 4.2792 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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