地沙双酮
地沙双酮用途
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。
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地沙双酮名称
[ CAS 号 ]:
702-54-5
[ 中文名 ]:
地沙双酮
[ 英文名 ]:
2H-1,3-Oxazine-2,4(3H)-dione,5,5-diethyldihydro-
[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
地沙双酮生物活性
[ 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 ]:
[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]
地沙双酮物理化学性质
[ 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
地沙双酮毒性和生态
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
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