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| Targets |
Methoxyphenamine hydrochloride targets β-adrenergic receptors. It acts as an agonist, stimulating these receptors to produce sympathomimetic effects. Its action in reducing histamine-induced nasal congestion is probably mediated, at least in part indirectly, with involvement of α1-adrenoceptors. By regulating the concentrations of norepinephrine and epinephrine, it modulates sympathetic nervous system activity.
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| ln Vitro |
In vitro, Methoxyphenamine hydrochloride functions as a β-adrenergic receptor agonist. Its activity is typically assessed by measuring its ability to stimulate cAMP accumulation in cells expressing β-ARs or by evaluating its relaxing effects on isolated smooth muscle preparations. As an amphetamine derivative, it may also have indirect sympathomimetic effects by promoting the release of endogenous catecholamines.
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| ln Vivo |
In vivo, Methoxyphenamine hydrochloride (1 mg kg-1, i.v.) inhibits histamine-induced nasal congestion in the rat. This sympathomimetic action in reducing nasal congestion is probably mediated, at least in part indirectly, with involvement of α1-adrenoceptors. It has been used as a bronchodilator, and its effects are consistent with the clinical use of β-adrenergic agonists for respiratory conditions.
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| Enzyme Assay |
For non-cell-based binding assays, Methoxyphenamine hydrochloride can be evaluated using membrane preparations from tissues expressing β-adrenergic receptors. Radioligand binding displacement experiments are performed using a radiolabeled antagonist such as [3H]-dihydroalprenolol. 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 propranolol. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing β-adrenergic receptors (e.g., CHO or HEK293 cells) or isolated tissue preparations (e.g., guinea pig trachea) are used. For cAMP accumulation assays, cells are treated with various concentrations of Methoxyphenamine hydrochloride, and cAMP levels are measured using ELISA or HTRF-based detection. For functional studies on smooth muscle, the compound's ability to relax pre-contracted tissue is assessed isometrically. The EC50 for relaxation or cAMP stimulation is calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, Methoxyphenamine hydrochloride can be administered to rodents via intravenous injection. In models of nasal congestion, the compound's ability to inhibit histamine-induced increases in nasal airway resistance is assessed. In models of bronchoconstriction, its bronchodilatory effects are evaluated by measuring lung function parameters. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Methoxyphenamine hydrochloride has a molecular weight of 215.72 and a molecular formula of C11H18ClNO. It is soluble in water and DMSO. The compound is a non-regulated analog of Methamphetamine. It is typically stored at room temperature in a cool, dry place. Its pharmacokinetic profile would be consistent with other sympathomimetic amines, with good oral absorption and metabolism in the liver.
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| Toxicity/Toxicokinetics |
The toxicity profile of Methoxyphenamine hydrochloride has not been extensively reported in the available literature. As a β-adrenergic agonist and amphetamine derivative, potential adverse effects may include tachycardia, hypertension, and central nervous system stimulation. 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.
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| Additional Infomation |
Methoxyphenamine hydrochloride is the hydrochloride salt of Methoxyphenamine, a β-adrenergic receptor agonist that regulates the concentrations of norepinephrine and epinephrine. It belongs to the amphetamine class of drugs and is a hydrochloride salt. It contains Methoxyphenamine.
Methoxyphenamine hydrochloride (NSC-65644) is a β-adrenergic receptor agonist that has been used clinically as a bronchodilator. It is a non-regulated analog of Methamphetamine and regulates the concentrations of norepinephrine and epinephrine. Its sympathomimetic action in reducing histamine-induced nasal congestion is probably mediated, at least in part indirectly, with involvement of α1-adrenoceptors. It is available for research purposes. |
| Molecular Formula |
C11H18CLNO
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| Molecular Weight |
215.72
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| Exact Mass |
215.107
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| CAS # |
5588-10-3
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| Related CAS # |
Methoxyphenamine;93-30-1
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| PubChem CID |
9859211
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| Appearance |
White to off-white solid powder
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| Density |
0.951 g/cm3
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| Boiling Point |
252.3ºCat 760 mmHg
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| Melting Point |
210°C
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| Flash Point |
102.6ºC
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| LogP |
3.038
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
138
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CC1=CC=CC=C1OC)NC.Cl
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| InChi Key |
FGSJNNQVSUVTPW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H17NO.ClH/c1-9(12-2)8-10-6-4-5-7-11(10)13-3;/h4-7,9,12H,8H2,1-3H3;1H
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| Chemical Name |
1-(2-methoxyphenyl)-N-methylpropan-2-amine;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) |
DMSO: ≥ 34 mg/mL (157.61 mM)
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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 | 4.6356 mL | 23.1782 mL | 46.3564 mL | |
| 5 mM | 0.9271 mL | 4.6356 mL | 9.2713 mL | |
| 10 mM | 0.4636 mL | 2.3178 mL | 4.6356 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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