Inhibition of14C-Aminopyrine accumulation in isolated rabbit gastric glands by the H2-receptor antagonist HOE 760 (TZU-0460)

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Abstract
Acid secretion in isolated rabbit gastric glands was measured by means of the14C-aminopyrine accumulation technique. Hoe 760 (TZU-0460) and Hoe 062, the desacetylated compound of Hoe 760, caused a concentration-dependent reduction of histamine (100 μM) induced aminopyrine-accumulation. The IC50-values were 3.16±0.84 μM (n=5) and 1.58±0.6 μM (n=6) for Hoe 760 and Hoe 062, respectively. In comparison an IC50 of 9.0±0.72 μM (n=6) was obtained for cimetidine and 3.3±1.4 μM (n=5) for ranitidine. The IC50-values of ranitidine, Hoe 760 and Hoe 062 were significantly different (p2-receptor antagonists.