S-2864(S-2864) - 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

Hoechst AG

在研机构-

非在研机构

Hoechst AG

最高研发阶段无进展药物发现

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C41H59N7O7

InChIKeyUOEDBDDWFLNBMX-NGLWMRMBSA-N

CAS号150739-46-1

关联

100 项与 S-2864 相关的临床结果

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100 项与 S-2864 相关的转化医学

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100 项与 S-2864 相关的专利（医药）

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1

项与 S-2864 相关的文献（医药）

1994-07-01·Arzneimittel-Forschung

Effects of the renin inhibitor N-[N-(3-(4-amino-1-piperidinyl-carbonyl)-2(R)-benzylpropionyl)-L- histid inyl] -(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6(2-pyridyl)-hexane-2-amide acetate in anesthetized rhesus monkeys.

Article

作者: Urbach, H ; Linz, W ; Schölkens, B A ; Jung, W ; Nickel, W U ; Ruppert, D ; Henning, R ; Heitsch, H ; Wagner, A ; Kleemann, H W

The renin inhibitory effect of the non-peptide renin inhibitor S 2864 (N-[N-(3-(4-Amino-1-piperidinyl-carbonyl)-2(R)-benzylpropionyl)-L- histidinyl]-(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6(2-pyridyl)-hexane-2- amide acetate, CAS 135683-92-0) was characterized in vitro and in vivo in primates. In vitro, S 2864 inhibited the activity of purified human plasma renin with an IC50 of 3.8 x 10(-10) mol/l and did not affect related human aspartyl proteases like human cathepsin E, cathepsin D or pepsin. In vivo, in anesthetized sodium depleted rhesus monkeys S 2864 decreased mean arterial blood pressure after intraduodenal (i.d.) administration of 2 mg/kg significantly by 27% from 94 +/- 8 to 62 +/- 6 mmHg for 90 min. Heart rate was not changed. Cumulative intravenous (i.v.) administration of S 2864 or remikiren in doses of 1, 10 and 30 micrograms/kg significantly decreased systemic blood pressure, dP/dtmax and cardiac output while heart rate was not changed. Plasma angiotensin II (ANG II) levels as well as renin activity were dose dependently reduced after 10, 30 and 60 min. It is concluded that S 2864 is an effective specific inhibitor of human renin eliciting marked blood pressure lowering activities in primates.

100 项与 S-2864 相关的药物交易

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