GR-70982(GR-70982) - 药物靶点：renin_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

renin

作用方式

抑制剂

作用机制

renin抑制剂(肾素抑制剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

高血压

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

权益机构-

最高研发阶段终止临床前

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C42H62N8O6

InChIKeySAJHPQMUYBTRMH-UHFFFAOYSA-N

CAS号124646-43-1

关联

100 项与 GR-70982 相关的临床结果

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100 项与 GR-70982 相关的转化医学

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100 项与 GR-70982 相关的专利（医药）

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1

项与 GR-70982 相关的文献（医药）

1991-01-01·European Journal of Pharmacology3区 · 医学

Acute and chronic effects of renin inhibitor GR70982 in the conscious marmoset

3区 · 医学

Article

作者: Peter C. Cherry ; Christopher J. Gardner ; David J. Twissell ; Peter A. Charlton

The effects on plasma renin activity (PRA), mean arterial blood pressure (MABP) and heart rate (HR) of GR70982, a low molecular weight inhibitor of human renin, were studied in conscious marmosets. In vitro, GR70982 is a potent and selective inhibitor of human plasma renin (concentration producing 50% inhibition (IC50): human renin = 6.9 x 10(-9) M; porcine pepsin and bovine cathepin D = greater than 10(-3) M). In normotensive marmosets, i.v. GR70982 (0.001-0.1 mg kg-1) produced a dose-related inhibition of PRA. Larger oral doses (0.2, 1 and 5 mg kg-1) were required to achieve similar effects. In renin-dependent hypertensive marmosets, i.v. GR70982 (0.01 and 0.5 mg kg-1) produced dose-related decreases in MABP (-12 and -18 mm Hg) and PRA (-93 and -100%), with only minimal effects on HR. A 7-day continuous i.v. infusion of GR70982 (0.36 mg kg-1 day-1) in sodium-deplete marmosets produced a gradual decrease in MABP (-17 mm Hg at day 7, cf. control), accompanied by an inhibition of PRA (approximately 75%) and minimal HR effects.

100 项与 GR-70982 相关的药物交易

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