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普啉索旦

普啉索旦用途

RGW2938 是一种磷酸二酯酶抑制剂。

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普啉索旦名称

[ CAS 号 ]:
111786-07-3

[ 中文名 ]:
普啉索旦

[ 英文名 ]:
RGW2938

[英文别名 ]:

Prinoxodanum
RGW 2938
Prinoxodanum [INN-Latin]
Prinoxodano [INN-Spanish]
PRINOXODAN
Prinoxodano
RGW2938

普啉索旦生物活性

[ 描述 ]:

RGW2938 是一种磷酸二酯酶抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 心血管疾病

[ 靶点 ]

Phosphodiesterase[1]

[体外研究]

RGW2938是一种口服有效的正性肌力/血管扩张剂。 RGW2938是一种新的非糖苷,非儿茶酚胺强心剂/血管扩张剂,可在离体豚鼠心脏中进行体外检测;在后者中,RGW2938 5 nmol-5μmol以剂量相关的方式增加收缩性[2]。

[体内研究]

RGW2938是一种新的非糖苷,非儿茶酚胺强心剂/血管扩张剂,在麻醉和清醒的狗体内进行体内检查。对麻醉的狗静脉内(iv)施用30-00μg/ kg的RGW2938以剂量相关的方式增加收缩力,同时降低动脉压和总外周阻力(TPR)。心率(HR)仅略微增加,并且主动脉血流没有明显改变。对有意识的慢性仪器化狗施用单次口服剂量的RGW2938 0.3mg/kg,在治疗后15-240分钟产生显着和持续的收缩性增加,同时仅略微增加HR。在美卡拉明-普萘洛尔诱导的心力衰竭模型中研究了RGW293830-300μg/ kg,iv的作用。 RGW2938通过增加心肌收缩力和降低动脉压有效地逆转药物引起的心力衰竭,同时仅略微影响HR [2]。

[参考文献]

[1]. Artigou JY, et al. [Evaluation of a new cardiotonic agent on human isolated atrium]. Ann Cardiol Angeiol (Paris). 1993 Feb;42(2):79-82.

[2]. Barrett JA, et al. Pharmacology of RG W-2938: a cardiotonic agent with vasodilator activity. J Cardiovasc Pharmacol. 1990 Oct;16(4):537-45.

[相关活性小分子]

普啉索旦物理化学性质

[ 密度 ]:
1.47g/cm3

[ 分子式 ]:
C₁₃H₁₃N₄O₂

[ 分子量 ]:
257.27

[ PSA ]:
73.80000

[ LogP ]:
1.11830

[ 折射率 ]:
1.724

[ 储存条件 ]:
-20°C，密闭，干燥

普啉索旦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA3144000

CHEMICAL NAME :: 2(1H)-Quinazolinone, 3,4-dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-py ridazinyl)-

CAS REGISTRY NUMBER :: 111786-07-3

LAST UPDATED :: 199512

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C13-H14-N4-O2

MOLECULAR WEIGHT :: 258.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990