EXPERIMENTAL STUDIES ON THE ANTITUSSIVE PROPERTIES OF THE NEW XANTHINE DERIVATIVE 1H-PURINE-2,6-DIONE, -3-METHYL-7[(5-METHYL-1,2,4-OXADIAZOL-3-YL)METHYL] - 2ND COMMUNICATION - INVESTIGATIONS ON THEOPHYLLINE-LIKE ACTIVITIES

CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3-methyl-7[(5-methy l-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) is a new xanthine der ivative, structurally related to theophylline. Potent antitussive acti vity in the 3 to 8 mg/kg dose range, by the oral route, was already de monstrated for this compound. In the present work, it is shown that co ntrary to theophylline. CH-13584 does not interact with adenosine A(1) receptor and is a weaker inhibitor of cyclic nucleotide phosphodieste rase. In addition, CH-13584 is a less active bronchodilator in vitro a nd in vivo. It is also devoid of the cardiovascular and behaviour side -effects of theophylline and of effects on diuresis at dosage well abo ve the antitussive dose. CH-13584, therefore has a different pharmacol ogical profile compared to theophylline and is devoid of the known sid e-effects of the latter. Such differences could result from a differen t biochemical profile.