雷佐生
雷佐生用途
消旋体为抗肿瘤药。用于辅助手术治疗，防止癌肿的转移，急性白血病，急性肉状细胞增多症，也可用于肺癌、胃癌、肝癌、乳腺癌及淋巴肉瘤等。(+)-构型用于cardioprotectant。用于乳腺癌患者的保护，和防止用蒽环类抗生素如阿霉素化疗时对心脏的副作用。
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雷佐生名称
[ CAS 号 ]:
21416-87-5
[ 中文名 ]:
雷佐生
[ 英文名 ]:
razoxane
[中文别名 ]:
[英文别名 ]:
- Zinecard
- ICRF-187
- Propane, (.+-.)-1,2-bis(3,5-dioxopiperazin-1-yl)-
- ICRF-159
- ICRF
- Eucardion
- Razoxane
- Razoxin
雷佐生物理化学性质
[ 密度 ]:
1.2576 (rough estimate)
[ 沸点 ]:
882.3ºC at 760 mmHg
[ 熔点 ]:
193ºC
[ 分子式 ]:
C11H16N4O4
[ 分子量 ]:
268.26900
[ 闪点 ]:
487.4ºC
[ 精确质量 ]:
268.11700
[ PSA ]:
98.82000
[ 蒸汽压 ]:
1.08E-31mmHg at 25°C
[ 折射率 ]:
1.6081 (estimate)
雷佐生毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- TL6400000
- CHEMICAL NAME :
- 2,6-Piperazinedione, 4,4'-propylenedi-, (+-)-
- CAS REGISTRY NUMBER :
- 21416-87-5
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 19
- MOLECULAR FORMULA :
- C11-H16-N4-O4
- MOLECULAR WEIGHT :
- 268.31
- WISWESSER LINE NOTATION :
- T6VMV ENTJ E3- ET6VMV ENTJ
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 81 mg/kg/3D-I
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting Blood - leukopenia Blood - thrombocytopenia
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 500 mg/kg
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting Blood - leukopenia Blood - thrombocytopenia
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 861 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 7488 mg/kg/52W-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Reproductive - Tumorigenic effects - uterine tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 15 gm/kg/Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Reproductive - Tumorigenic effects - uterine tumors
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 12 gm/kg/Y-I
- TOXIC EFFECTS :
- Tumorigenic - Carcinogenic by RTECS criteria Blood - lymphoma, including Hodgkin's disease
- TYPE OF TEST :
- TD - Toxic dose (other than lowest)
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1 gm/kg/8W-I
- TOXIC EFFECTS :
- Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 37500 ug/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 37500 ug/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 30 mg/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- DOSE :
- 37500 mg/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 10 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 15 mg/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- DOSE :
- 2520 mg/kg
- SEX/DURATION :
- male 42 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Paternal Effects - testes, epididymis, sperm duct
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 105 mg/kg
- SEX/DURATION :
- female 6-8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
MUTATION DATA
- TYPE OF TEST :
- Mutation in mammalian somatic cells
- TEST SYSTEM :
- Rodent - mouse Lung
- DOSE/DURATION :
- 200 ug/L
- REFERENCE :
- MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 157,199,1985
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雷佐生制备
1. 100g的1,2-丙二胺四乙酸和400ml甲酰胺，在氮气保护下，于100～110℃共热1h，再于150-155℃共热4h。所成的棕色的溶液在减压下，于80-90℃下蒸去溶剂。剩余物溶入120ml甲醇，在冰箱中放置过夜。过滤，用甲醇洗，在65℃下真空干燥，得到62g淡米黄色的雷佐生细微结晶，收率70%，熔点237～239℃。
2. 在反应瓶中加入1,2-丙二胺四乙酸(1,2-diaminopropane-N,N,N,N-tetraacetic acid) 100g(0.326mol)和甲酰胺NH2COH 400ml(10.01mol),搅拌混合,于N2保护下在100~110ºC搅拌反应1h,再升温至150~155ºC,在该温度下搅拌反应4h.棕色反应液于80~90ºC下减压蒸除溶剂,剩余物加入甲醇120ml,置于冰箱中过夜.析出结晶,过滤,滤饼用甲醇洗,65ºC下真空干燥,得雷佐生淡米黄色结晶62g,收率70%,mp237~239ºC.
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