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The adenosine A 2B  receptor is a critical protein in intestinal water secretion. In the present study, we screened compound libraries to identify inhibitors of the A 2B  receptor and evaluated their effect on adenosine-induced intestinal fluid secretion. The screening identified the dihydropyridine calcium antagonists nifedipine and nisoldipine. Their respective affinities for the A 2B  receptor ( K  i  value) were 886 and 1,399 nM. Nifedipine and nisoldipine, but not amlodipine or nitrendipine, inhibited both calcium mobilization and adenosine-induced cAMP accumulation in cell lines. Moreover, adenosine injection into the lumen significantly increased fluid volume in the colonic loop of wild-type mice but not A 2B  receptor-deficient mice. PSB-1115, a selective A 2B  receptor antagonist, and nifedipine prevented elevated adenosine-stimulated fluid secretion in mice. Our results may provide useful insights into the structure–activity relationship of dihydropyridines for A 2B  receptor. As colonic fluid secretion by adenosine seems to rely predominantly on the A 2B  receptor, nifedipine could be a therapeutic candidate for diarrhoea-related diseases.

A2B adenosine receptor inhibition by the dihydropyridine calcium channel blocker nifedipine involves colonic fluid secretion