Studies on the inhibitory action of leminoprazole against rabbit gastric H+,K+-ATPase.

Masuda, Makoto; Uchida, Aoi; Matsukura, Hitoshi; Kamishiro, Toshiro

doi:10.1254/fpj.104.325

Cited by 3 publications

(1 citation statement)

References 24 publications

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“…In contrast, omeprazole had no effect on any cell damage, as described previously [7], It is well established that omeprazole is rapid ly converted to its active sulfenamide form within the acidic compartment, and then reacts with thiol groups of the gastric acid pump [16], Likewise, the inhibition of acid pump activity by leminoprazole is greater at a lower pH, and thus it is speculated that lemi noprazole combines with enzyme thiol groups through some activated reactions under acidic conditions [17], However, the culture medium used here was buffered at neutral pH with a bicarbonate-CCL system, so neither of these drugs might be changed. Overall, it is suggested that unchanged leminoprazole might be effective in the prevention of cell damage, but unchanged omeprazole has no effect.…”

Section: Discussionmentioning

confidence: 60%

Leminoprazole Protects Cultured Gastric Mucosal Cells against Damage Caused by Ethanol, Indometacin and Taurocholate

Takahashi¹,

Yamazaki²,

Okabe³

1997

Pharmacology

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We examined whether or not leminoprazole (an acid pump inhibitor) protects cultured rabbit gastric mucosal cells against various forms of cell damage. Exposure of mucosal cells to ethanol, indometacin or taurocholate for 1 h caused a reduction in their viability. Pretreatment of the cells with leminoprazole for 2 h concentration-dependently and significantly prevented the viability loss induced by each noxious agent, although the drug alone did not affect cell viability. Cytoprotection by leminoprazole was expressed after a 2-hour lag period. The effects of leminoprazole were potently inhibited by cycloheximide and actinomycin D. These results indicate that leminoprazole directly acts on gastric mucosal cells, making the cells resistant to damage, and that its cytoprotection might be mediated through de novo synthesized proteins.

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Section: Discussionmentioning

confidence: 60%

Leminoprazole Protects Cultured Gastric Mucosal Cells against Damage Caused by Ethanol, Indometacin and Taurocholate

Takahashi¹,

Yamazaki²,

Okabe³

1997

Pharmacology

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Benzimidazole derivatives: Spectrum of pharmacological activity and toxicological properties (a review)

et al. 1999

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Inhibitory Effect of Leminoprazole on Acid Secretion in Parietal Cells Isolated from Guinea Pig Gastric Mucosa

Saito

Matsuo

1995

Japanese Journal of Pharmacology

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ABSTRACT-Isolated guinea pig parietal cells, the function of which is similar to that of human parietal cells, were used in this study. The accumulation of 14C-aminopyrine (14C-AP) was measured to study the inhibitory mechanism of leminoprazole in cells. Stimulation by 10 pM histamine, 0.1 mM carbachol, 1 pM gastrin or 1 mM db-cAMP brought about satisfactory incorporation of 14C-AP, and leminoprazole concentration-dependently inhibited acid secretion induced by these stimulants. At 10-5 M, almost 100% inhibition was observed. The IC50 values of leminoprazole obtained from its inhibitory action on histamine, carbachol, gastrin and db-cAMP-stimulated acid secretion were 4.0 x 10-7 M, 3.5 x 10-7 M, 2.5 x 10-7 M and 5.6 x 10-7 M, respectively. Thus the extent of inhibition was the same for the responses to all the secretagogues. These results indicate that the site of action of leminoprazole is intracellular and distal from cAMP (intracellular second messenger), but not at the receptor sites. The results also strongly suggest that the inhibitory action of leminoprazole on H+, K+-ATPase may contribute to the inhibitory effect of this drug on gastric acid secretion.

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Studies on the inhibitory action of leminoprazole against rabbit gastric H+,K+-ATPase.

Cited by 3 publications

References 24 publications

Leminoprazole Protects Cultured Gastric Mucosal Cells against Damage Caused by Ethanol, Indometacin and Taurocholate

Leminoprazole Protects Cultured Gastric Mucosal Cells against Damage Caused by Ethanol, Indometacin and Taurocholate

Benzimidazole derivatives: Spectrum of pharmacological activity and toxicological properties (a review)

Inhibitory Effect of Leminoprazole on Acid Secretion in Parietal Cells Isolated from Guinea Pig Gastric Mucosa

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