Methoxyphenamine hydrochloride
Based on 1 Customer Validation
Methoxyphenamine hydrochloride (NSC-65644) is a bronchodilator. Methoxyphenamine hydrochloride exhibits α- and β-adrenergic receptor agonist effects. Methoxyphenamine hydrochloride reduces basal nasal resistance and inhibits Histamine (HY-B1204)-induced nasal congestion. Methoxyphenamine hydrochloride undergoes metabolism mediated by CYP2D6. Methoxyphenamine hydrochloride can be used in research related to nasal congestion and bronchial asthma.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 5588-10-3
- Formula: C11H18ClNO
- Molecular Weight:215.72
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
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α adrenergic receptor |
β-adrenoceptor |
CYP2D6 |
Methoxyphenamine (95 μM; 24-96 h) hydrochloride is metabolized by P4502D6-transfected h2D6v2 cells via O-dealkylation, aromatic hydroxylation, and N-demethylation pathways, with ~30% metabolism achieved by 72 h, while control cHol cells show no metabolism of the compound[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Methoxyphenamine hydrochloride (1-10 mg/kg; intravenous injection) dose-dependently inhibits histamine (HY-B1204)-induced nasal congestion in anesthetized male Wistar rats, with an ID50 of 1.16 mg/kg against nasal congestion induced by 0.2% histamine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 300-450 g, anaesthetized with basal nasal resistance)[1]
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Dosage:0.01-30 mg/kg
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Administration:i.v.
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Result:Caused a dose-dependent reduction in nasal basal resistance, indicated by decreased ventilation overflow.
Was less potent and less efficacious than adrenaline but produced longer-lasting decongestant responses (>15 minutes).
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Animal Model:Wistar (male, 300-450 g, anaesthetized, histamine-induced nasal congestion)[1]
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Dosage:1-10 mg/kg (histamine-induced congestion inhibition); 1 mg/kg (after prazosin/desmethylimipramine pretreatment)
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Administration:i.v.; cumulative doses after histamine challenge
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Result:Caused a dose-dependent reduction in histamine-induced nasal congestion.
Achieved an ID50 of 1.16 mg/kg for inhibition of 0.2% histamine-induced congestion and an ID50 of 1.9 mg/kg for inhibition of 2% histamine-induced congestion.
Produced longer-lasting effects than adrenaline.
Had its log dose-response curve shifted significantly rightward by prazosin pretreatment (degree of shift: 2.3 for 0.1 mg/kg prazosin, 7.48 for 0.3 mg/kg prazosin).
Had its log dose-response curve shifted significantly rightward by desmethylimipramine pretreatment (degree of shift: 1.75 for 0.1 mg/kg desmethylimipramine, 2.96 for 1 mg/kg desmethylimipramine).
Chemical Information
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CAS No. 5588-10-3
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Appearance Solid
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Molecular Weight 215.72
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Formula C11H18ClNO
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Color White to off-white
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SMILES
COC1=CC=CC=C1CC(C)NC.[H]Cl
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Synonyms
NSC-65644
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (463.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lau WA, et al. Methoxyphenamine inhibits basal and histamine-induced nasal congestion in anaesthetized rats. British journal of pharmacology. 1990 Oct;101(2):394-8. [Content Brief]
[2]. Geertsen S, et al. Metabolism of methoxyphenamine and 2-methoxyamphetamine in P4502D6-transfected cells and cell preparations. Xenobiotica; the fate of foreign compounds in biological systems. 1995 Sep;25(9):895-906. [Content Brief]
[3]. Thevis M, et al. Doping control analysis of methoxyphenamine using liquid chromatography-tandem mass spectrometry. European journal of mass spectrometry (Chichester, England). 2008;14(3):145-52. [Content Brief]
[4]. Phillis JW, et al. The effect of alpha-, beta adrenergic receptor agonists and antagonists on the efflux of 22Na and uptake of 42K by rat brain cortical slices. Brain Res. 1982 Mar 18;236(1):133-42. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6356 mL | 23.1782 mL | 46.3564 mL | 115.8910 mL |
| 5 mM | 0.9271 mL | 4.6356 mL | 9.2713 mL | 23.1782 mL | |
| 10 mM | 0.4636 mL | 2.3178 mL | 4.6356 mL | 11.5891 mL | |
| 15 mM | 0.3090 mL | 1.5452 mL | 3.0904 mL | 7.7261 mL | |
| 20 mM | 0.2318 mL | 1.1589 mL | 2.3178 mL | 5.7945 mL | |
| 25 mM | 0.1854 mL | 0.9271 mL | 1.8543 mL | 4.6356 mL | |
| 30 mM | 0.1545 mL | 0.7726 mL | 1.5452 mL | 3.8630 mL | |
| 40 mM | 0.1159 mL | 0.5795 mL | 1.1589 mL | 2.8973 mL | |
| 50 mM | 0.0927 mL | 0.4636 mL | 0.9271 mL | 2.3178 mL | |
| 60 mM | 0.0773 mL | 0.3863 mL | 0.7726 mL | 1.9315 mL | |
| 80 mM | 0.0579 mL | 0.2897 mL | 0.5795 mL | 1.4486 mL | |
| 100 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 1.1589 mL |
Methoxyphenamine hydrochloride Related Classifications
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