FPL-62129(FPL-62129) - 药物靶点：L-type calcium channel_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

L-type calcium channel

作用机制

L-type calcium channel阻滞剂(L-型电压门控性钙通道家族阻滞剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

高血压心肌缺血

原研机构

阿斯利康制药有限公司

在研机构-

非在研机构

阿斯利康制药有限公司Fisons Plc

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C20H19ClF5NO4

InChIKeyOBWJAVIHPMZUHG-UHFFFAOYSA-N

CAS号95445-79-7

关联

100 项与 FPL-62129 相关的临床结果

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100 项与 FPL-62129 相关的转化医学

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100 项与 FPL-62129 相关的专利（医药）

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1

项与 FPL-62129 相关的文献（医药）

1988-03-01·Journal of Cardiovascular Pharmacology4区 · 医学

Cardiovascular Profile of FPL 62129, a Novel Dihydropyridine Calcium Channel Blocker, in Anaesthetised Dogs

4区 · 医学

Article

作者: O'Connor, S. E. ; Humphries, R. G.

The cardiovascular effects of FPL 62129, a novel dihydropyridine calcium channel blocker, were studied in chloralose-anaesthetised dogs in comparison with those of nifedipine. FPL 62129 and nifedipine produced dose-related falls in blood pressure and total peripheral resistance and were of similar potency in these respects. While the vasodilator effects of nifedipine were accompanied by reflex tachycardia, FPL 62129 reduced blood pressure without altering heart rate. Both compounds increased cardiac contractility and cardiac output. Nifedipine reduced PR interval duration of the ECG, whereas FPL 62129 produced no change. These differences between FPL 62129 and nifedipine are reflections of their respective cardiac profiles. In studies performed after cardiac autonomic block (to eliminate the contribution from reflexes), FPL 62129 showed marked activity at the sinus node and to a lesser extent at the atrioventricular node. Unlike nifedipine, FPL 62129 demonstrates vasodilator and direct decelerator properties over the same dose range, which accounts for its ability to lower blood pressure without causing reflex tachycardia in this model. The observed profile of FPL 62129 questions attempts to classify calcium channel blockers of the dihydropyridine type as selective vasodilators.

100 项与 FPL-62129 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
高血压	临床2期	英国	Fisons Plc	-
高血压	临床2期	-	阿斯利康制药有限公司	-
心肌缺血	临床前	-	阿斯利康制药有限公司	-
心肌缺血	临床前	英国	Fisons Plc	-