303-34-4

• 常用中文名：毛果天芥菜碱
• 常用英文名：Lasiocarpine
• CAS号：303-34-4
• 分子式：C₂₁H₃₃NO₇
• 分子量：411.489
• 相关类别： 研究领域 癌症
• 发布时间：2018-02-20 08:00:00
• 更新时间：2024-01-16 10:30:55
• 拉索卡品是一种肝毒性吡咯利嗪生物碱(PA),在体内可引起致命的肝静脉闭塞性疾病。只有在其代谢转化为有毒中间体(包括脱氢罗拉西平和N-氧化物)后,罗拉西平才具有毒性[1]。

名称

• 中文名: 毛果天芥菜碱
• 英文名: lasiocarpine
• 中文别名: 毛果天芥菜鹼
• 英文别名: (1S,7aR)-7-[({(2S)-2,3-dihydroxy-2-[(1S)-1-methoxyethyl]-3-methylbutanoyl}oxy)methyl]-2,3,5,7a-tetrahydro-1H-pyrrolizin-1-yl (2Z)-2-methylbut-2-enoate (non-preferred name); Lasiocarpin; (1S,7aR)-7-[({(2S)-2,3-Dihydroxy-2-[(1S)-1-methoxyethyl]-3-methylbutanoyl}oxy)methyl]-2,3,5,7a-tetrahydro-1H-pyrrolizin-1-yl (2Z)-2-methyl-2-butenoate

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 519.8±50.0 °C at 760 mmHg
• 熔点: 97ºC
• 分子式: C₂₁H₃₃NO₇
• 分子量: 411.489
• 闪点: 268.1±30.1 °C
• 精确质量: 411.225708
• PSA: 105.53000
• LogP: 2.85
• 外观性状: 无色至米色结晶固体
• 蒸汽压: 0.0±3.1 mmHg at 25°C
• 折射率: 1.545

生物活性

• 描述: 拉索卡品是一种肝毒性吡咯利嗪生物碱(PA),在体内可引起致命的肝静脉闭塞性疾病。只有在其代谢转化为有毒中间体(包括脱氢罗拉西平和N-氧化物)后,罗拉西平才具有毒性[1]。
• 相关类别:
  研究领域 >> 癌症
• 体外研究: 只有在其代谢转化为有毒中间体(称为脱氢罗拉西卡品[1])后,拉西卡品才具有毒性。脱氢罗拉西平和其他假定的二氢吡咯里西啶生物碱(吡咯酯)非常活泼,它们攻击DNA和蛋白质等亲核大分子,引发严重毒性,包括肝静脉阻塞性疾病和肿瘤[1]。拉西阿品在体外主要通过五种代谢途径进行代谢,即脱氢、酯键断裂和去甲基化[1]。
• 参考文献:

  [1]. Muluneh M Fashe, et al. Species-Specific Differences in the in Vitro Metabolism of Lasiocarpine. Chem Res Toxicol. 2015 Oct 19;28(10):2034-44.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OE7875000 CHEMICAL NAME : Lasiocarpine CAS REGISTRY NUMBER : 303-34-4 LAST UPDATED : 199803 DATA ITEMS CITED : 32 MOLECULAR FORMULA : C21-H33-N-O7 MOLECULAR WEIGHT : 411.55 WISWESSER LINE NOTATION : T55 AN CUTJ D1OVXQXQ1&1&Y1&O1 FOVY1&U2 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 : 110 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 78 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 88 mg/kg TOXIC EFFECTS : Liver - other changes TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 80 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 72 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 85 mg/kg TOXIC EFFECTS : Liver - other changes TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 20 mg/kg TOXIC EFFECTS : Liver - other changes TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - hamster DOSE/DURATION : 67500 ug/kg TOXIC EFFECTS : Liver - other changes TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 255 mg/kg/2Y-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 470 mg/kg/56W-I TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Skin and Appendages - tumors TYPE OF TEST : TD - Toxic dose (other than lowest) ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 546 mg/kg/2Y-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma TYPE OF TEST : TD - Toxic dose (other than lowest) ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1310 mg/kg/2Y-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma TYPE OF TEST : TD - Toxic dose (other than lowest) ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 760 mg/kg/48W-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Skin and Appendages - tumors TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Heritable translocation test TYPE OF TEST : DNA inhibition TYPE OF TEST : Mutation test systems - not otherwise specified MUTATION DATA TYPE OF TEST : Cytogenetic analysis TEST SYSTEM : Mammal - species unspecified Leukocyte DOSE/DURATION : 25 umol/L REFERENCE : CYTBAI Cytobios. (Faculty Press, 88 Regent St., Cambridge, UK) V.1- 1969- Volume(issue)/page/year: 14,151,1975 *** REVIEWS *** IARC Cancer Review:Animal Sufficient Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,281,1976 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,281,1976 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,1171,1976

安全

• 危险品运输编码: UN 1544
• 包装等级: III
• 危险类别: 6.1(b)