| Description | Leminoprazole is an orally available H+,K(+)-ATPase inhibitor that protects gastric mucosal cells from various cellular damages. |
| In vitro | Leminoprazole浓度依赖性地抑制了H+, K(+)-ATPase的活性，其IC50值在pH 7.4时为31 μM。[1] |
| In vivo | Leminoprazole dose-dependently inhibited the H+, K(+)-ATPase activity at 3 and 6 hr after the administration at 10-100 mg/kg, p.o. Leminoprazole (60 mg/kg, p.o.) inhibited the H+, K(+)-ATPase activity persistently, and the duration of its inhibitory action was much longer than that of omeprazole (30 mg/kg, p.o.). In pylorus-ligated rats, good correlations between the respective inhibitory rates against gastric acid output and H+, K(+)-ATPase activity were found after the administration of Leminoprazole. These results suggest that Leminoprazole inhibits gastric acid secretion by its ability to inhibit the H+, K(+)-ATPase activity in rats; its inhibitory activity was comparable to that of omeprazole. In addition, Leminoprazole (100 mg/kg) inhibited the H+, K(+)-ATPase activity even when administered intragastrically after pylorus-ligation, suggesting that this drug can inhibit H+, K(+)-ATPase activity directly from the gastric lumen. Moreover, Leminoprazole (100 mg/kg, p.o.) when administered repeatedly for 2 or 4 weeks inhibited the H+, K(+)-ATPase activity to the same degree as the single administration.[1] |
| Target activity | K+-ATPase:31 μM |
| molecular weight | 341.47 |
| Molecular formula | C19H23N3OS |
| CAS | 104340-86-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (146.43 mM) |
| References | 1. Matsukura H, et al. Effect of a new antiulcer drug, leminoprazole, on the gastric mucosal H+,K(+)-ATPase activity in rats. Nihon Yakurigaku Zasshi. 1994 Aug;104(2):91-100. 2. Takahashi S, et al. Effects of acid-degraded products of leminoprazole on acid secretion, mucus secretion and synthesis, and indomethacin-induced damage in cell culture. J Physiol Pharmacol. 1998 Mar;49(1):99-110. 3. Okabe S, et al. Antisecretory effect of leminoprazole on histamine-stimulated gastric acid secretion in dogs: potent local effect. Jpn J Pharmacol. 1995 Oct;69(2):91-100. 4. Takahashi S, et al. The cytoprotective effect of leminoprazole on indomethacin-induced damage to rabbit gastric mucosal cells. J Pharmacol Exp Ther. 1996 Nov;279(2):975-82. |