702-54-5

• 常用中文名：地沙双酮
• 常用英文名：2H-1,3-Oxazine-2,4(3H)-dione,5,5-diethyldihydro-
• CAS号：702-54-5
• 分子式：C₈H₁₃NO₃
• 分子量：171.19
• 相关类别： 研究领域 神经疾病
• 发布时间：2018-09-22 05:47:15
• 更新时间：2024-01-29 09:53:12
• 二氧酮是一种具有惊厥性质的物质,在性质上类似于轻氮唑和苯甲酰脲。二氧酮具有口服活性。

名称

• 中文名: 地沙双酮
• 英文名: 5,5-diethyl-1,3-oxazinane-2,4-dione
• 英文别名: Dietadione [Italian]; Diethadione; Dioxone; Persisten; 5,5-diethyldihydro-2H-1,3-oxazine-2,4(3H)-dione; 5,5-Diaethyl-dihydro-[1,3]oxazin-2,4-dion; Toce; 5,5-diethyl-[1,3]oxazinane-2,4-dione; DIETHADION; Tocen; Lepton; Ledosten; Dietroxin; 5,5-diethyl-dihydro-[1,3]oxazine-2,4-dione

物化性质

• 密度: 1.069g/cm3
• 分子式: C₈H₁₃NO₃
• 分子量: 171.19
• 精确质量: 171.09000
• PSA: 55.40000
• LogP: 1.38800
• 折射率: 1.44

生物活性

• 描述: 二氧酮是一种具有惊厥性质的物质,在性质上类似于轻氮唑和苯甲酰脲。二氧酮具有口服活性。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 体外研究: 二氧酮可溶于乙醇、乙醚、氯仿和丙二醇。可在pH值为4.3的室温下获得1%的水溶液,并在升温至50℃时制备2%的水溶液[1]。
• 体内研究: 二氧酮(0-30毫克/千克；静脉注射,静脉注射,口服,皮下注射；一次)诱导惊厥作用[1]。动物模型：CF-1小鼠和CF-Wistar大鼠【1】剂量：0-30 mg/kg给药：腹腔注射,一次结果：小鼠自发活动常减少,10 mg/kg时常伴有高反应性,给药30 mg/kg后出现震颤、阵挛性惊厥和运动不协调现象。大鼠：10 mg/kg时可观察到肢体肌肉震颤和部分孤立性阵挛,15 mg/kg以上时可出现阵挛性惊厥。
• 参考文献:

  [1]. G MAFFII, et al. A new analeptic: 5, 5-diethyl-1, 3-oxazine-2,4-dione (Dioxone). J Pharm Pharmacol. 1961 Apr;13:244-53.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RP6300000 CHEMICAL NAME : 2H-1,3-Oxazine-2,4(3H)-dione, 5,5-diethyldihydro- CAS REGISTRY NUMBER : 702-54-5 BEILSTEIN REFERENCE NO. : 0133129 LAST UPDATED : 199701 DATA ITEMS CITED : 10 MOLECULAR FORMULA : C8-H13-N-O3 MOLECULAR WEIGHT : 171.22 WISWESSER LINE NOTATION : T6OVMVTJ E2 E2 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 71 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 32 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 39 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 81 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,282,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 49 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,281,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 61 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,281,1970 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 32 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 45 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : RPOBAR Research Progress in Organic-Biological and Medicinal Chemistry. (New York, NY) V.1-3, 1964-72. Discontinued. Volume(issue)/page/year: 2,282,1970 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 4550 mg/kg/26W-I TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Related to Chronic Data - death REFERENCE : JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 13,244,1961