| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
| Targets |
Norfenefrine hydrochloride targets α1-adrenergic receptors. As an agonist, it binds to and activates these G protein-coupled receptors, leading to vasoconstriction and increased peripheral resistance. It is structurally related to norepinephrine. By stimulating α1-ARs, it increases blood pressure and causes vasoconstriction in various vascular beds. It may also have some activity at β-adrenergic receptors.
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| ln Vitro |
In vitro, Norfenefrine hydrochloride acts as an α1-adrenergic receptor agonist. Its activity is typically assessed by measuring its ability to stimulate calcium mobilization or contraction in cells or tissues expressing α1-ARs. The compound's potency and efficacy as an α1-agonist can be determined and compared to reference agonists like phenylephrine. It may also have some activity at β-adrenergic receptors.
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| ln Vivo |
In vivo, Norfenefrine hydrochloride produces effects consistent with α1-adrenoceptor activation, including vasoconstriction and increased blood pressure. It has been used clinically as a nasal decongestant and in the treatment of hypotension. Its pressor effects are mediated through stimulation of α1-adrenergic receptors on vascular smooth muscle. However, comprehensive in vivo pharmacological studies are limited.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Norfenefrine hydrochloride can be evaluated using membrane preparations from cells expressing human α1-adrenergic receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-prazosin. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled prazosin. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human α1-adrenergic receptors are cultured in appropriate media. For functional assays, intracellular calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and treated with various concentrations of Norfenefrine hydrochloride. Fluorescence intensity is measured using a fluorescence plate reader. The increase in calcium signal compared to control wells indicates agonist activity. EC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, Norfenefrine hydrochloride can be administered to rodents via intravenous or intraperitoneal injection. In cardiovascular studies, blood pressure and heart rate are monitored following compound administration. In models of nasal congestion, its vasoconstrictor effects on nasal mucosa are assessed. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
Norfenefrine hydrochloride has a molecular weight of 189.64 and a molecular formula of C8H12ClNO2. It is structurally related to norepinephrine. The compound is typically stored under recommended conditions. It is soluble in water and DMSO. It is for research use only and is not intended for human consumption outside of approved clinical indications.
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| Toxicity/Toxicokinetics |
The toxicity profile of Norfenefrine hydrochloride includes potential for hypertension, tachycardia, and cardiac arrhythmias at high doses due to its vasoconstrictor effects. The compound is for research use only and is not intended for human consumption outside of approved clinical indications. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of cardiovascular function.
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| References |
[1]. Tracheal phenol red secretion, a new method for screening mucosecretolytic compounds. J Pharmacol Methods. 1984 Jun;11(3):151-7.
[2]. Acute effect of norfenefrine on the urethral pressure profile in females with genuine stress incontinence. Urol Int. 1991;46(2):176-9. |
| Additional Infomation |
Norfenefrine hydrochloride belongs to the phenolic compound class.
Norfenefrine hydrochloride is a sympathomimetic agent and α1-adrenergic receptor agonist. It is structurally related to norepinephrine and acts as a vasoconstrictor and pressor agent. It has been used clinically as a nasal decongestant and in the treatment of hypotension. It is available for research purposes only. |
| Molecular Formula |
C8H12CLNO2
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|---|---|
| Molecular Weight |
189.64
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| Exact Mass |
189.055
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| CAS # |
4779-94-6
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| Related CAS # |
Norfenefrine;536-21-0
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| PubChem CID |
3016408
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| Appearance |
White to off-white solid powder
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| Density |
1.249g/cm3
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| Boiling Point |
360.7ºC at 760mmHg
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| Melting Point |
162-164ºC(lit.)
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| Flash Point |
172ºC
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| LogP |
1.886
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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 |
2
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| Heavy Atom Count |
12
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| Complexity |
119
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)O)C(CN)O.Cl
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| InChi Key |
OWMFSWZUAWKDRR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H11NO2.ClH/c9-5-8(11)6-2-1-3-7(10)4-6;/h1-4,8,10-11H,5,9H2;1H
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| Chemical Name |
3-(2-amino-1-hydroxyethyl)phenol;hydrochloride
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| Synonyms |
norfenefrine hydrochloride; 4779-94-6; Norfenefrine HCl; Zondel; DTXSID1046710;
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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 (e.g. under nitrogen), 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 | 5.2731 mL | 26.3657 mL | 52.7315 mL | |
| 5 mM | 1.0546 mL | 5.2731 mL | 10.5463 mL | |
| 10 mM | 0.5273 mL | 2.6366 mL | 5.2731 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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