299-39-8

• 常用中文名：硫酸金雀花碱
• 常用英文名：Sparteine sulfate pentahydrate
• CAS号：299-39-8
• 分子式：C₁₅H₂₈N₂O₄S
• 分子量：332.46
• 相关类别： 原料药 循环系统用药 抗心律失常药
• 发布时间：2018-03-15 08:00:00
• 更新时间：2024-01-11 18:19:16
• 能降低心肌应激性和传导性，减慢心率，抑制心脏收缩力。主要用于室性心动过速和功能性心悸，为子宫有收缩作用，亦可用于催产和子宫出血等，亦用于配制人工冬眠疗法、冬眠合剂等。

名称

• 中文名: 硫酸司巴丁
• 英文名: sparteine sulfate
• 中文别名: 硫酸金雀花碱
• 英文别名: (7α,9α)-Sparteine sulfate (1:1); Sparteinsulfat; (-)-Spartein,Sulfat; spartocin; Sparteine, sulfate; 7,14-Methano-2H,6H-dipyrido[1,2-a:1',2'-e][1,5]diazocine, dodecahydro-, (7R,7aR,14R,14aS)-, sulfate (1:1); spareng; sparteine mono(hydrogen sulfate); sparteal; (-)-sparteine,sulfate; (1S,2R,9S,10S)-7,15-Diazatetracyclo[7.7.1.0.0]heptadecansulfat; (1S,2R,9S,10S)-7,15-Diazatetracyclo[7.7.1.0.0]heptadecane sulfate; 7,14-Methano-2H,6H-dipyrido[1,2-a:1',2'-e][1,5]diazocine, dodecahydro-, (7S,7aR,14S,14aS)-, sulfate (1:1); Sparteine sulfate (VAN); [7S; sparm; Sparteine, sulfate (1:1); spartin; spartein sulfate pentahydrate; Sparteine sulfate anhydrous; spatym; Spartea; spartepur; (1S,2R,9S,10S)-7,15-Diazatétracyclo[7.7.1.0.0]heptadécane sulfate; Sparteine Sulfate; spal; L-Spartein sulfat; Sparteine sulfate (1:1)

物化性质

• 沸点: 340.9ºC at 760mmHg
• 熔点: 135ºC
• 分子式: C₁₅H₂₈N₂O₄S
• 分子量: 332.46
• 闪点: 148.3ºC
• 精确质量: 332.176971
• PSA: 89.46000
• LogP: 2.64890
• 外观性状: 无色结晶或白色结晶性粉末
• 蒸汽压: 2.61E-11mmHg at 25°C
• 储存条件: -20°C

生物活性

• 描述: (-)-Sparteine (sulfate) 是一种可以从 Lupinus 中提取的喹啉西啶生物碱。(-)-Sparteine (sulfate) 抑制乙酰胆碱的释放,具有抗惊厥作用。
• 相关类别:
  信号通路 >> 跨膜转运 >> 胆碱受体
  信号通路 >> 神经信号通路 >> 胆碱受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Villalpando-Vargas F, et al. Sparteine as an anticonvulsant drug: Evidence and possible mechanism of action. Seizure. 2016 Jul;39:49-55.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : WG6430000 CHEMICAL NAME : Sparteine, sulfate CAS REGISTRY NUMBER : 299-39-8 LAST UPDATED : 199007 DATA ITEMS CITED : 10 MOLECULAR FORMULA : C15-H26-N2.H2-O4-S MOLECULAR WEIGHT : 332.51 WISWESSER LINE NOTATION : T C66 K66 A HN PNTJ &WSQQ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 30400 ug/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - stiffness Behavioral - muscle contraction or spasticity REFERENCE : JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 16,353,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 350 mg/kg TOXIC EFFECTS : Behavioral - excitement REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1497,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 43 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 20,1668,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 117 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - stiffness Behavioral - muscle contraction or spasticity REFERENCE : JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 16,353,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 15 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - stiffness Behavioral - muscle contraction or spasticity REFERENCE : JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 16,353,1966 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 80 mg/kg TOXIC EFFECTS : Vascular - regional or general arteriolar or venous dilation REFERENCE : JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,431,1926 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 42 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JAGRAC Journal of Agricultural Research (Washington, DC). (Washington, DC) V.1-78, 1913-49. Discontinued. Volume(issue)/page/year: 32,51,1926 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Amphibian - frog DOSE/DURATION : 375 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 27,431,1926 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 3 mg/kg SEX/DURATION : female 39 week(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - parturition REFERENCE : AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 105,304,1969 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 6 mg/kg SEX/DURATION : female 39 week(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - stillbirth REFERENCE : AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 89,263,1964

安全

• 风险声明 (欧洲): 23/25-33
• 安全声明 (欧洲): 1-45
• 危险品运输编码: UN 1544
• 包装等级: III
• 危险类别: 6.1(b)