Characterization of a Novel Potassium-Competitive Acid Blocker of the Gastric H,K-ATPase, 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine Monofumarate (TAK-438)

Inhibition of the gastric H,K-ATPase by the potassium-competitive acid blocker (P-CAB) 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine (TAK-438), is strictly K(+)-competitive with a K(i) of 10 nM at pH 7. In contrast to previous P-CABs, this structure has a point p...

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Autores principales: Shin, Jai Moo, Inatomi, Nobuhiro, Munson, Keith, Strugatsky, David, Tokhtaeva, Elmira, Vagin, Olga, Sachs, George
Formato: Artigo
Lenguaje:Inglês
Publicado: The American Society for Pharmacology and Experimental Therapeutics 2011
Materias:
Gastrointestinal, Hepatic, Pulmonary, and Renal
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC3199995/
https://ncbi.nlm.nih.gov/pubmed/21828261
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/jpet.111.185314
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