Pharmacological characterization of the postjunctional beta-adrenoceptors in the rat gastric fundus.

In order to characterize the postjunctional beta-adrenoceptors in the rat gastric fundus, we studied the influence of beta-agonists and beta-antagonists on methacholine-contracted fundus strips. The mixed beta-agonist isopropylnoradrenaline and the beta 2-selective agonist fenoterol had a concentration-dependent relaxing effect and at higher concentrations completely inhibited the methacholine-induced tone. The reputedly beta 1-selective agonist prenalterol only produced about 50% inhibition and another reputedly beta 1-selective agonist, tazolol, had almost no relaxing effect. The beta-antagonists propranolol (beta 1 + beta 2), practolol (beta 1), H35/25 (beta 2) and ICI 118,551 (beta 2) all shifted the concentration-response curves for isopropylnoradrenaline and fenoterol in a parallel way to the right, but the slope of the Schild plot was not significantly different from 1 only for the antagonism of isopropylnoradrenaline by H35/25. The relaxing effect of prenalterol was only clearly antagonized by ICI 118,551. The results suggest that postjunctional beta 1- and beta 2-adrenoceptors are present in the rat gastric fundus.