夸西泮
夸西泮用途
【用途一】
具有苯并二氮杂卓类典型的抗焦虑、抗惊厥和肌松作用，且毒性很低。用于各种失眠症。
具有苯并二氮杂卓类典型的抗焦虑、抗惊厥和肌松作用，且毒性很低。用于各种失眠症。
夸西泮名称
[ CAS 号 ]:
36735-22-5
[ 中文名 ]:
夸西泮
[ 英文名 ]:
Quazepam
[中文别名 ]:
[英文别名 ]:
- EINECS 253-179-4
- Prosedar
- Cetrane
- Quazium
- Oniria
- Dormalin
- DORAL
- Quazepam
- Selepam
- Quazepamum
夸西泮物理化学性质
[ 密度 ]:
1.4±0.1 g/cm3
[ 沸点 ]:
429.9±55.0 °C at 760 mmHg
[ 熔点 ]:
22°C
[ 分子式 ]:
C17H11ClF4N2S
[ 分子量 ]:
386.794
[ 闪点 ]:
213.8±31.5 °C
[ 精确质量 ]:
386.026764
[ PSA ]:
47.69000
[ LogP ]:
4.06
[ 蒸汽密度 ]:
>1 (vs air)
[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C
[ 折射率 ]:
1.595
夸西泮毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- DE9710000
- CHEMICAL NAME :
- 2H-1,4-Benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1- (2,2,2-trifluoroethyl)-
- CAS REGISTRY NUMBER :
- 36735-22-5
- BEILSTEIN REFERENCE NO. :
- 0901084
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 10
- MOLECULAR FORMULA :
- C17-H11-Cl-F4-N2-S
- MOLECULAR WEIGHT :
- 386.81
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 :
- >5 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 2749 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- LDLo - Lowest published 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 :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 32,1456,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 845 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Lungs, Thorax, or Respiration - respiratory depression
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - cat
- DOSE/DURATION :
- >1 gm/kg
- TOXIC EFFECTS :
- Behavioral - ataxia Behavioral - analgesia
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 32,1456,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Primate - monkey
- DOSE/DURATION :
- 18 gm/kg/52W-I
- TOXIC EFFECTS :
- Liver - fatty liver degeneration Liver - changes in liver weight Related to Chronic Data - death
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - hamster
- DOSE/DURATION :
- 14 gm/kg/4W-I
- TOXIC EFFECTS :
- Liver - changes in liver weight Related to Chronic Data - changes in ovarian weight
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 90 mg/kg
- SEX/DURATION :
- female 13-21 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 520 mg/kg
- SEX/DURATION :
- female 6-18 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 37,906,1987
夸西泮安全信息
[ 危险品运输编码 ]:
3249
[ 包装等级 ]:
III
[ 危险类别 ]:
6.1(b)
夸西泮上下游产品
夸西泮上游产品
夸西泮下游产品
夸西泮制备
7-氯-1-(2,2,2-三氟乙基)-2,3-二氢-5-(2-氟苯基)-1,4-苯并二氮杂卓(I) 用四氧化钌或三氧化铬氧化，得化合物(Ⅱ)。1.8g(0.005mo1)化合物(1I)溶于20ml无水二氧六环，加入1.1g(0.005mo1)五硫化磷，沸腾回流4h(装置上装有氯化钙干燥管，以防空气中的湿气侵入)。减压浓缩，剩余物溶于二氯甲烷，用装有200g的硅胶柱过滤。滤液浓缩后，用二氯甲烷-己烷重结晶，得1.2g夸西泮，熔点137.5～139℃。
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