Universal adenosine receptor antagonism is neither necessary nor desirable with xanthine antiasthmatics

Abstract

The great diversity of pharmacological effects of xanthines may well reflect different cellular mechanisms of action. Major attention is presently devoted to adenosine receptor antagonism that, in contrast to phosphodiesterase inhibition, is clearly produced by therapeutic concentrations of theophylline. The ubiquitous adenosine effects together with the universal and potent blocking action of methylxanthines have led investigators to believe that most pharmacological actions including antiasthmatic effects of theophylline reflect adenosine antagonism. The present hypothesis proposes that universal adenosine receptor antagonism is neither necessary nor desirable with xanthine antiasthmatics. Supporting the hypothesis a xanthine derivative that seems to be devoid of functional effects at important adenosine receptor sites has been shown to be a potent bronchodilator drug that lacks theophylline-like diuretic and CNS-stimulant behavioural effects.