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- Title
A Substituted Thieno[3.4-d]imidazole versus Substituted Benzimidazoles as H<sup>+</sup>, K<sup>+</sup>-ATPase Inhibitors.
- Authors
Herling, A.W.; Bickel, M.; Lang, H.-J.; Weidmann, K.; Rösner, M.; Metzger, H.; Rippel, R.; Nimmesgern, H.; Scheunemann, K.-H.
- Abstract
S 3337, 2-(2-ethylaminobenzylsulfinyl)-5,6-dimethoxybenzimidazole, and S 1924, 2-(5-methyl-2-picolylsulfιnyl)-1H-thieno[3.4-d]imidazole, are members of new classes of H+, K+-ATPase inhibitors. Their effects on H+, K+-ATPase and 14C-aminopyrine uptake in gastric glands were studied as well as in vivo in pylorus-ligated rats, stomach-lumen-perfused rats and Heidenhain pouch dogs. Their inhibitory effects were compared with the effect of omeprazole. In pylorus-ligated rats the two compounds showed a similar effectiveness as omeprazole. In stomach-lumen-perfused rats and in particular in Heidenhain pouch dogs, S 3337 was clearly less effective than omeprazole, while S 1924 was similarly effective in all in vivo models and in the H+, K+-ATPase assay as omeprazole. The difference in potency between S 1924 and omeprazole on 14C-aminopyrine uptake in gastric glands can be explained by the lower pKa value of S 1924 (3.4) than that of omeprazole (4.0). Additionally, this study shows that there was no correlation between the effects in rats, particularly in pylorus-ligated rats, and in dogs for the H+, K+-ATPase inhibitors tested. It is concluded from this study that substituted thieno[3.4-d]imidazoles represent a new class of potent gastric acid inhibitors. Copyright © 1988 S. Karger AG, Basel
- Publication
Pharmacology, 1988, Vol 36, Issue 5, p289
- ISSN
0031-7012
- Publication type
Article
- DOI
10.1159/000138397