Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells.
Open Access
- 1 June 1983
- Vol. 24 (6) , 557-560
- https://doi.org/10.1136/gut.24.6.557
Abstract
The inhibitory effect of the three benzimidazole derivatives timoprazole, picoprazole, and omeprazole on histamine and dbcAMP stimulated 14C-aminopyrine accumulation (= H+ secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibited H+ secretion in a concentration dependent manner with IC50 values of 8.5 +/- 1.9 mumol/l for timoprazole, 3.9 +/- 0.7 mumol/l for picoprazole, and 0.13 +/- 0.03 mumol/l for omeprazole. The IC50 of timoprazole, when dbcAMP was used as a stimulus, did not differ significantly from that of histamine stimulation. The type of inhibition was of a non-competitive nature. The full acid response to histamine after temporary exposure of the cells to the benzimidazoles could be restored by washing the cells twice; this suggests that the inhibition is reversible. The data - among others - indicate that the properties of the benzimidazoles described here would allow these compounds to be used as effective antisecretagogues.This publication has 5 references indexed in Scilit:
- Isolation of brush-border membrane from the rabbit descending colon epithelium. Partial characterization of a unique K+-activated ATPase.Journal of Biological Chemistry, 1981
- Substituted benzimidazoles inhibit gastric acid secretion by blocking (H+ + K+) ATPaseNature, 1981
- The Actions of Secretagogues on Oxygen Uptake by Isolated Mammalian Parietal CellsJournal of Clinical Investigation, 1978
- On the Evaluation of the Constants Vm and KM in Enzyme ReactionsScience, 1952
- On the Evaluation of the Constants
V
m
and
K
M
in Enzyme ReactionsScience, 1952