3438. Doxofylline

Nomenclature

CAS number: 69975-86-6
7-(1,3-Dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione; 7-(1,3-dioxolan-2-ylmethyl)theophylline; 2-(7′-theophyllinemethyl)-1,3-dioxolane; doxophylline; dioxyfilline; ABC-12/3; Ansimar (ABC); Ventax (Yamanouchi).
C11H14N4O4; mol wt 266.25.
C 49.62%, H 5.30%, N 21.04%, O 24.04%.

Description and references

Prepn: U. Avico et al., Farmaco Ed. Sci. 17, 73 (1962). Use as bronchodilator: BE 868556; J. S. Franzone, T. Tamietto, US 4187308 (1978, 1980 to Istituto Biologico Chemioterapico ABC). Pharmacology: J. S. Franzone et al., Farmaco Ed. Sci. 36, 201 (1981). HPLC determn in plasma: A. Lagana et al., Biomed. Chromatogr. 4, 205 (1990). Clinical pharmacokinetics: E. Bologna et al., J. Int. Med. Res. 18, 282 (1990). Review of pharmacology and clinical efficacy in patients with heart disease: F. L. Dini, R. Cogo, Curr. Med. Res. Opin. 16, 258-268 (2001).

Chemical structure

Properties

Crystals, mp 144-145.5°. Sol in water, acetone, ethyl acetate, benzene, chloroform, dioxane, hot methanol or hot ethanol. Practically insol in ethyl ether or petr ether. LD50 in mice (mg/kg): 841 orally; 215.6 i.v.; in rats: 1022.4 orally, 445 i.p. (Franzone).

Therapeutic Category

Bronchodilator.

Keywords

Bronchodilator; Xanthine Derivatives