B-844-39(B-844-39) - 药物靶点：ADRA1 x 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

ADRA1 x L-type calcium channel

作用机制

ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、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

原研机构

Takeda Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Takeda Pharmaceutical Co., Ltd.

最高研发阶段终止临床1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C36H40ClN3O6

InChIKeyMHOSUIMBPQVOEU-UHFFFAOYSA-N

CAS号119934-51-9

查看全部结构式(2)

关联

100 项与 B-844-39 相关的临床结果

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100 项与 B-844-39 相关的转化医学

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100 项与 B-844-39 相关的专利（医药）

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1

项与 B-844-39 相关的文献（医药）

1987-09-01·Journal of Cardiovascular Pharmacology4区 · 医学

Antihypertensive Effects of Niguldipine-HCl (B 844–39), a New Calcium Antagonist in Dogs

4区 · 医学

Article

作者: Krumpl, G. ; Mayer, N. ; Raberger, G. ; Schneider, W. ; Fischer, G.

B 844-39 is a new dihydropyridine calcium antagonist with a long-lasting antihypertensive action. Preliminary tests in chronically instrumented normotensive dogs revealed that B 844-39 (0.3 mg/kg p.o.) caused a marked decrease in blood pressure which was accompanied by a counterregulatory increase in heart rate. Both effects outlasted the 6-h observation period. There was no sign of cardiac depression in left ventricular positive dP/dtmax or sonomicrometrically evaluated subendocardial systolic shortening. B 844-39 was also tested in renal hypertensive dogs over a period of 12 days to investigate its potential in the long-term treatment of hypertension. A dosage of 0.3 mg/kg given orally twice a day led to a marked and persistent decrease in blood pressure, which was accompanied by a positive chronotropic effect and increases in plasma renin activity and angiotensin II. This initial counterregulatory response was blunted within several days of chronic treatment. After completion of the 12-day treatment period, the blood pressure reduction persisted for greater than 14 days. B 844-39 induced a marked and persistent reduction in blood pressure in hypertensive dogs, even with prolongation of the dosing interval to 24 h. The hypotensive effect of this drug was more pronounced in hypertensive than in normotensive animals.

100 项与 B-844-39 相关的药物交易

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