(CP-66948)-药物靶点：H2 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

CP 66948

靶点

H2 receptor(组胺H2受体)

作用机制

H2 receptor拮抗剂(组胺H2受体拮抗剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

胃溃疡

原研机构

Pfizer Inc.

在研机构-

非在研机构

Pfizer Inc.

最高研发状态(全球)无进展临床1期

首次获批日期(全球)-

最高研发状态(中国)-

特殊审评-

结构

分子式C13H20N6S

InChIKeyOZSXWXGDJLBJQO-UHFFFAOYSA-N

CAS号101189-47-3

关联

100 项与 CP-66948 相关的专利（医药）

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1

项与 CP-66948 相关的文献（医药）

1991-12-01·Digestive Diseases and Sciences3区 · 医学

CP-66,948: an antisecretory histamine H₂-receptor antagonist with mucosal protective properties

3区 · 医学

Article

作者: Hakkinen, John P. ; Holt, William F. ; Goddard, Carl J. ; Oates, Peter J. ; Murphy, William R. ; Maciejko, James J. ; Reiter, Lawrence A.

CP-66,948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties. The affinity of CP-66,948 for the guinea pig atria histamine H2-receptor is 15 times greater than that of cimetidine and seven times greater than that of ranitidine. In vivo, the ED50 value for inhibition of gastric acid secretion in pylorus-ligated rats is 2 mg/kg intraduodenally, and in histamine or pentagastrin-stimulated Heidenhain pouch dogs the antisecretory ED50 values are 0.3 mg/kg per os and 1.0 mg/kg per os, respectively. CP-66,948 also inhibits ethanol-induced gastric hemorrhagic lesions in rats following either oral or systemic administration (ED50 values of 12 mg/kg per os and 6 mg/kg subcutaneously). In addition, the mucosal protective activity is independent of prostaglandin synthesis. CP-66,948 inhibits gastric acid secretion in man, and its mucosal protective activity may provide additional benefits in peptic ulcer therapy.