<Originals>Pharmacological and toxicological study of newly synthesized 1,3-dimethylxanthine derivatives

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Two originally 7-basic substituted theophylline derivatives from theophylline sodium salt, dichloroalkane and N-methyl-N-cyclohexyl amine were synthesized and their pharmacological activities in guinea pigs and rats were studied. The acute toxicity (LD_<50>) of the compounds was determined in mice and rats by the method of Litchfield and Wilcoxon, using a personal Pravetz 8M computer. A comparative pharmacological study on the in vivo bronchodilatory effects and in vitro tracheal relaxant action of the synthesized compounds with aminophylline was performed in guinea pigs. The inhibition of cyclic AMP-phosphodiesterase (PDE) in the heart and lungs of rats by these compounds was compared to that by theophylline. The newly synthesized compounds had in vivo and in vitro bronchodilatory and diuretic activities, and exerted a marked inhibitory effect on the cyclic AMP-PDE in lung homogenates of rats. These findings indicate that the substitutions with a shorter carbonic chain at the 7-position could improve the bronchodilatory effect of methylxanthines.
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