WY-26769(WY-26769) - 药物靶点：Proton pump_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

Proton pump

作用方式

抑制剂

作用机制

质子泵抑制剂

治疗领域

消化系统疾病

在研适应症-

非在研适应症

消化性溃疡

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

权益机构-

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C14H11N3S

InChIKeyHNQWIEGVHZAQOC-UHFFFAOYSA-N

CAS号96733-58-3

关联

100 项与 WY-26769 相关的临床结果

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100 项与 WY-26769 相关的转化医学

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100 项与 WY-26769 相关的专利（医药）

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1

项与 WY-26769 相关的文献（医药）

1991-01-01·Drug Development Research

Gastric antisecretory activity of an acid stable H⁺/K⁺ ATPase inhibitor, WY‐26,769

作者: Roger Crossley ; George J. Palumbo ; John F. DiJoseph ; Arthur A. Santilli ; Susan T. Nielsen

AbstractWY‐26,769 (2‐3‐dihydro‐2‐(2‐pyridinyl) thiazolo‐[3,2‐a]benzimidazole) is a gastric antisecretory agent that acts by inhibiting the parietal cell proton pump. In vitro, WY‐26,769 was active against dbcAMP‐stimulated aminopyrine uptake in isolated parietal cells. Preincubating the drug with liver microsomal enzymes increased its potency 50 times, to an IC50 of 6.8 μM. Wy‐26,769 and its oxidative metabolite Wy‐26,876 each inhibited the H+/K+ ATPase (IC50 = 42 μM and 18 μM, respectively). In whole animal studies, Wy‐26,769 inhibited histaminestimulated gastric acid secretion (ID50 = 3 mg/kg) irrespective of whether Wy‐26,769 was administered orally or intravenously. Wy‐26,769 was not degraded in acid and also inhibited gastric acid secretion in the pylorus‐ligated rat. Wy‐26,769 was equiactive after oral or intravenous administration demonstrating that it is an acid stable proton pump inhibitor.

100 项与 WY-26769 相关的药物交易

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