Doxapram HCl

Catalog No.S4037 Batch:S403701

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Technical Data

Formula

C24H30N2O2.HCl.H2O

Molecular Weight 432.98 CAS No. 7081-53-0
Solubility (25°C)* In vitro DMSO 87 mg/mL (200.93 mM)
Water 25 mg/mL (57.73 mM)
Ethanol 2 mg/mL (4.61 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
Targets
TASK-1 [1] TASK-1/TASK-3 heterodimeric [1] TASK-3 [1]
410 nM(EC50) 9 μM(EC50) 37 μM(EC50)
In vitro Doxapram inhibits both TASK-1 and TASK-3 function in a dose dependent manner. Doxapram inhibition at both hyperpolarized and depolarized potentials, as well as effects independent of extracellular potassium concentration. It is said that the carboxy terminal domain of TASK-1 is important to doxapram inhibition. Doxapram also inhibits TRESK, TASK-2, and TREK-1 but at significantly larger concentrations (EC50s of 240 μM, 460 μM, and >1 mM, respectively). Doxapram has no effect on MAC for halothane. [1]
In vivo Doxapram is an analeptic agent. The respiratory stimulant action is manifested by an increase in tidal volume associated with a slight increase in respiratory rate. A pressor response may result following Doxapram administration. The mean half-life is 3.4 h (range 2.4-4.1h), the mean apparent volume of distribution is 1.5 mg/kg and the whole body clearance is 370 mL/min. Enteric-coated capsules of doxapram base are absorbed rapidly after an initial delay, and the systemic availability is about 60%.[2]

Protocol (from reference)

Animal Study:

[3]

  • Animal Models

    male Japanese white rabbits

  • Dosages

    0.25 mg/kg/h, 0.50 mg/kg/h

  • Administration

    Infusion

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.