Doxofylline

Catalog No.S4164 Synonyms: Doxophylline

For research use only.

Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.

Doxofylline Chemical Structure

CAS No. 69975-86-6

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Biological Activity

Description Doxofylline (Doxophylline) is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.
Targets
PDE [1]
In vitro

Doxofylline has PDE inhibitor activity and can increase the level of cAMP, which could, therefore, be used for the treatment of asthma and COPD. EC50 value of Doxofylline is 15 times higher than that of aminophylline in inhibiting the adenosine-induced relaxation of tracheal smooth muscle and 10 times higher in reducing the negative inotropic effect induced by adenosine on isolated guinea-pig atria. Doxofylline could effectively decrease the open probability of the calcium-activated potassium channels as a result of both the shortening of open period and the prolongation of close time. Doxofylline has greatly decreased affinity towards adenosine A1 and A2 receptors when compared with theophylline, which may contribute to the better safety profile. Moreover, unlike theophylline, Doxofylline does not interfere with calcium influx into cells nor antagonizes the action of calcium-channel blockers. [1]

In vivo Doxofylline has been shown to have better efficacy with fewer side effects than theophylline. 30 mg/kg Doxofylline increases heart rate of anaesthetized cat by 13 beats/min. The effective therapeutic dose of Doxofylline has less cardio-stimulant effects than Theophylline, such that Doxofylline does not out significantly increase the cardiac frequency nor does it have arrhythmogenic effects. [2]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 266.25
Formula

C11H14N4O4

CAS No. 69975-86-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CC3OCCO3

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