Doxapram hydrochloride hydrate
Based on 1 publication(s) in Google Scholar
Doxapram hydrochloride hydrate is a respiratory stimulant. Doxapram hydrochloride hydrate increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram hydrochloride hydrate inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram hydrochloride hydrate significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram hydrochloride hydrate can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity.
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- Pureté : 99.28%
- CAS No.: 7081-53-0
- Formule: C24H33ClN2O3
- Masse moléculaire:432.98
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Doxapram hydrochloride hydrate
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Activité biologique
Description
In Vitro
Doxapram hydrochloride hydrate (0.01-100 μM, 10-30 min) inhibits human and porcine TASK-1 with IC50s of 0.88 and 0.93 μM in human and porcine atrial muscle cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Doxapram hydrochloride hydrate (> 1 mg/kg, i.v.) stimulates the brainstem respiratory center rather than the peripheral chemoreceptors in dogs[4].
Doxapram hydrochloride hydrate (1-2 mg/kg, i.v., single dose or once daily for 14 days) has a specific anti-arrhythmic effect on the atrium in domestic pigs[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute atrial fibrillation and persistent atrial fibrillation models established in domestic pigs[6]
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Dosage:1 and 2 mg/kg (single dose) and 2 mg/kg (continuous administration)
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Administration:Intravenous injection (i.v.), single dose or once daily for 14 days
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Result:Prolonged the effective refractory period of the atrium (AERP), but has no effect on ventricular repolarization.
Reversed the electrical remodeling associated with AF (increased TASK-1 current and shortened APD) in long-term treatment.
Chemical Information
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CAS No. 7081-53-0
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Appearance Solid
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Masse moléculaire 432.98
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Formule C24H33ClN2O3
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Color White to off-white
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SMILES
O=C1N(CC)CC(CCN2CCOCC2)C1(C3=CC=CC=C3)C4=CC=CC=C4.Cl.O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (115.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (57.74 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Cotten JF, et al. The ventilatory stimulant doxapram inhibits TASK tandem pore (K2P) potassium channel function but does not affect minimum alveolar anesthetic concentration. Anesth Analg, 2006, 102(3), 779-785. [Content Brief]
[2]. Anderson-Beck, R., et al., Doxapram stimulates dopamine release from the intact rat carotid body in vitro. Neurosci Lett, 1995. 187(1): p. 25-8. [Content Brief]
[3]. Peers, C., Effects of doxapram on ionic currents recorded in isolated type I cells of the neonatal rat carotid body. Brain Res, 1991. 568(1-2): p. 116-22. [Content Brief]
[4]. Yost CS. A new look at the respiratory stimulant doxapram. CNS Drug Rev. 2006 Fall-Winter;12(3-4):236-49. [Content Brief]
[5]. Vliegenthart RJ, et al. Doxapram Treatment for Apnea of Prematurity: A Systematic Review. Neonatology. 2017;111(2):162-171. doi: 10.1159/000448941. Epub 2016 Oct 20. [Content Brief]
[6]. Wiedmann F, et al. Treatment of atrial fibrillation with doxapram: TASK-1 potassium channel inhibition as a novel pharmacological strategy. Cardiovasc Res. 2022 Jun 22;118(7):1728-1741. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3096 mL | 11.5479 mL | 23.0958 mL | 57.7394 mL |
| 5 mM | 0.4619 mL | 2.3096 mL | 4.6192 mL | 11.5479 mL | |
| 10 mM | 0.2310 mL | 1.1548 mL | 2.3096 mL | 5.7739 mL | |
| 15 mM | 0.1540 mL | 0.7699 mL | 1.5397 mL | 3.8493 mL | |
| 20 mM | 0.1155 mL | 0.5774 mL | 1.1548 mL | 2.8870 mL | |
| 25 mM | 0.0924 mL | 0.4619 mL | 0.9238 mL | 2.3096 mL | |
| 30 mM | 0.0770 mL | 0.3849 mL | 0.7699 mL | 1.9246 mL | |
| 40 mM | 0.0577 mL | 0.2887 mL | 0.5774 mL | 1.4435 mL | |
| 50 mM | 0.0462 mL | 0.2310 mL | 0.4619 mL | 1.1548 mL | |
| DMSO | 60 mM | 0.0385 mL | 0.1925 mL | 0.3849 mL | 0.9623 mL |
| 80 mM | 0.0289 mL | 0.1443 mL | 0.2887 mL | 0.7217 mL | |
| 100 mM | 0.0231 mL | 0.1155 mL | 0.2310 mL | 0.5774 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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