Home Transmembrane Transporters Potassium Channel inhibitor Doxapram HCl For research use only.

Doxapram HCl

Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

Doxapram HCl Chemical Structure

Doxapram HCl Chemical Structure

CAS: 7081-53-0

Purity & Quality Control

Batch: Purity: 99.75%
99.75

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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
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
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]
Animal Research Animal Models male Japanese white rabbits
Dosages 0.25 mg/kg/h, 0.50 mg/kg/h
Administration Infusion
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03894189 Unknown status Weaning Failure Beni-Suef University May 2019 Not Applicable
NCT02421068 Completed Premature Birth Sinno H.P. Simons|ZonMw: The Netherlands Organisation for Health Research and Development|Leiden Amsterdam Centre for Drug Research (LACDR)|Dutch Knowledge Centre for Pediatric Pharmacotherapy (NKFK)|Centre for Human Drug Research Netherlands|Radboud University Medical Center|Erasmus Medical Center August 2014 --
NCT00389909 Completed Premature Infants|Apnea Jean Michel Hascoet|Maternite Regionale Universitaire November 2006 Phase 4

Chemical lnformation & Solubility

Molecular Weight 432.98 Formula

C24H30N2O2.HCl.H2O
CAS No. 7081-53-0 SDF Download Doxapram HCl SDF
Smiles CCN1CC(C(C1=O)(C2=CC=CC=C2)C3=CC=CC=C3)CCN4CCOCC4.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (200.93 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 25 mg/mL

Ethanol : 2 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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