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Chemical Compound Review:

TY 11345 sodium2-(1H-benzoimidazol-2- ylsulfinyl)-8...

Synonyms:

Yamaguchi, T. et al., Uematsu, T. et al.

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Disease relevance of 2-(1H-benzoimidazol-2-ylsulfinyl)-8-methoxy-11-azabicyclo[5.4.0]undeca-8,12-diene

These results suggest that TY-11345 has potent antisecretory and antiulcer effects which are exerted by suppression of H+/K(+)-ATPase activity in gastric parietal cells, so that TY-11345 should be useful for the clinical treatment of peptic ulcer diseases [1].

High impact information on 2-(1H-benzoimidazol-2-ylsulfinyl)-8-methoxy-11-azabicyclo[5.4.0]undeca-8,12-diene

The pharmacokinetics and safety of TY-11345 [(+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt], a novel gastric proton pump inhibitor, were studied in healthy male volunteers after single (20, 40, and 80 mg) and repeated oral doses (60 mg, once daily for 7 days) as enteric-coated tablet [2].
The effect of food intake on the pharmacokinetic parameters of TY-11345, which was evaluated at the dose of 40 mg in a cross-over design, was not significant [2].
In pylorus ligated rats, TY-11345 inhibited basal gastric acid secretion by both the intraduodenal and oral routes, with ED50 values of 1.2 and 4.0 mg/kg, respectively [1].
Moreover, the antisecretory effect of TY-11345 persisted for more than 24 hr in pylorus ligated rats [1].
TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes; and the inhibitory effect was enhanced under weak acid conditions, the IC50 (concentrations that inhibit the enzyme activity by 50%) being 5.8 microM and 9.9 microM at pH 6.0 and pH 7.4, respectively [1].

Anatomical context of 2-(1H-benzoimidazol-2-ylsulfinyl)-8-methoxy-11-azabicyclo[5.4.0]undeca-8,12-diene

We investigated the effects of the newly synthesized proton pump inhibitor TY-11345, (+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin- 9-yl)sulfinyl]-1H-benzimidazole sodium salt, on gastric mucosal proton pump (H+/K(+)-ATPase) activity, gastric acid secretion and gastro-duodenal lesions in experimental animals [1].

References

Biochemical and pharmacological properties of a newly synthesized proton pump (H+/K(+)-ATPase) inhibitor, TY-11345 in experimental animals. Yamaguchi, T., Aihara, K., Yamada, S., Narita, S., Kogi, K. Jpn. J. Pharmacol. (1993) [Pubmed]
Pharmacokinetic properties of a novel gastric proton pump inhibitor, (+/-)-2-[(4-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)sulfinyl]-1H-benzimidazole sodium salt, in healthy subjects. Uematsu, T., Nakano, M., Kosuge, K., Nagai, A., Sato, A., Nakashima, M. Journal of pharmaceutical sciences. (1994) [Pubmed]

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