Effects of the adenosine A1-receptor antagonist on defecation, small intestinal propulsion and gastric emptying in rats.

We examined the effects of 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) and (R)-7,8-dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1 -i]purin- 5(4H)-one (KF20274), selective adenosine A1-receptor antagonists, on the gastrointestinal propulsion in rats, as compared with those of the laxative bisacodyl. DPCPX and KF20274 (p.o.) dose-dependently increased the fecal pellet output, whereas these drugs at the dose that increased defecation did not affect small intestinal propulsion or gastric emptying. Bisacodyl increased defecation and slowed gastric emptying without any influence on small intestinal propulsion. Bisacodyl, but not DPCPX or KF20274, induced diarrhea at the dose inducing defecation. The present results suggest that the adenosine A1-receptor antagonist selectively enhances the lower gastrointestinal propulsion, resulting in defecation without diarrhea.