111786-07-3

• 常用中文名：普啉索旦
• 常用英文名：RGW2938
• CAS号：111786-07-3
• 分子式：C₁₃H₁₃N₄O₂
• 分子量：257.27
• 相关类别： 信号通路 代谢酶/蛋白酶 磷酸二酯酶(PDE)
• 发布时间：2018-06-05 08:00:00
• 更新时间：2024-01-02 22:26:08
• RGW2938 是一种磷酸二酯酶抑制剂。

名称

• 中文名: 普啉索旦
• 英文名: 3-methyl-6-(6-oxo-4,5-dihydro-1H-pyridazin-3-yl)-1,4-dihydroquinazolin-2-one
• 英文别名: Prinoxodanum; RGW 2938; 3,4-Dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2(1H)-quinazolinone; Prinoxodanum [INN-Latin]; Prinoxodano [INN-Spanish]; PRINOXODAN; 2(1H)-Quinazolinone,3,4-dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl); Prinoxodano; RGW2938

物化性质

• 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

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.

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