[CAS NO. 7081-53-0] Doxapram HCl

Name: Doxapram HCl
Brand: Arctom Scientific
SKU: SLK-S4037

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PRODUCTS SPECIFICATIONS [7081-53-0]

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Catalog

SLK-S4037

Brand

Selleck

CAS

7081-53-0

DESCRIPTION [7081-53-0]

Overview

MDL	MFCD09954698
Molecular Weight	432.98
Molecular Formula	C24H30N2O2.HCl.H2O
SMILES	C(CN1CCOCC1)C2C(C(=O)N(CC)C2)(C3=CC=CC=C3)C4=CC=CC=C4.Cl.O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3096 mL	11.5479 mL	23.0958 mL
5 mM	0.4619 mL	2.3096 mL	4.6192 mL
10 mM	0.2310 mL	1.1548 mL	2.3096 mL
50 mM	0.0462 mL	0.2310 mL	0.4619 mL

Description

Doxapram HCl inhibits heterodimeric channel function with 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.

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%.

References

[1] Cotten JF, et al. Anesth Analg, 2006, 102(3), 779-785.
[2] Robson RH, et al. Br J Clin Pharmacol, 1979, 7(1), 81–87.
[3] Okuyama K, et al. Anesth Analg, 2003, 97(3), 759-762.

Synonyms

2-Pyrrolidinone, 1-ethyl-4-[2-(4-morpholinyl)ethyl]-3,3-diphenyl-, hydrochloride, hydrate (1:1:1)

2-Pyrrolidinone, 1-ethyl-4-(2-morpholinoethyl)-3,3-diphenyl-, monohydrochloride, monohydrate

2-Pyrrolidinone, 1-ethyl-4-[2-(4-morpholinyl)ethyl]-3,3-diphenyl-, monohydrochloride, monohydrate

AHR 619

Doxapram hydrochloride hydrate

1-Ethyl-4-(2-morpholinoethyl)-3,3-diphenyl-2-pyrrolidinone hydrochloride hydrate

Doxapram hydrochloride monohydrate

1-Ethyl-4-[2-(morpholin-4-yl)ethyl]-3,3-diphenylpyrrolidin-2-one hydrate hydrochloride