86-34-0

• 常用中文名：苯琥胺
• 常用英文名：Phensuximide
• CAS号：86-34-0
• 分子式：C₁₁H₁₁NO₂
• 分子量：189.21100
• 相关类别： 医药中间体 杂环化合物 吡啶类化合物 碘吡啶
• 发布时间：2018-03-22 08:00:00
• 更新时间：2024-01-08 11:13:36
• Phensuximide 是一种琥珀酰亚胺类抗癫痫 (antiepileptic) 和抗惊厥 (anticonvulsant) 试剂。Phensuximide 可以抑制去极化脑组织中 cyclic AMP 和 cyclic GMP 的积累。在动物模型中,Phensuximide 可用于癫痫治疗的相关研究。

名称

• 中文名: 苯琥胺
• 英文名: phensuximide
• 中文别名: 米浪丁
• 英文别名: 1-methyl-3-phenyl-pyrrolidine-2,5-dione; 1-methyl-3-phenylsuccinimide; Milontin; Lifen; Mirotin; Lifene; Mirontin; 1-Methyl-3-phenyl-pyrrolidin-2,5-dion; Milonton; Epimal; Epimid; N-methylphenylsuccinimide; PM 334

物化性质

• 密度: 1.1596 (rough estimate)
• 沸点: 324.47°C (rough estimate)
• 熔点: 71-73°
• 分子式: C₁₁H₁₁NO₂
• 分子量: 189.21100
• 精确质量: 189.07900
• PSA: 37.38000
• LogP: 1.09680
• 折射率: 1.5012 (estimate)
• 储存条件: 2-8°C

生物活性

• 描述: Phensuximide 是一种琥珀酰亚胺类抗癫痫 (antiepileptic) 和抗惊厥 (anticonvulsant) 试剂。Phensuximide 可以抑制去极化脑组织中 cyclic AMP 和 cyclic GMP 的积累。在动物模型中,Phensuximide 可用于癫痫治疗的相关研究。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
  研究领域 >> 神经疾病
• 靶点:

  IC50: cyclic AMP and cyclic GMP accumulation[2]

• 体外研究: 苯苏肟在小鼠大脑皮层的孵育切片中产生去极化诱导的环GMP或环AMP水平积累,ID50值为8.00 mM或6.20 mM[2]。苯妥英钠(0.5-2.0mm)具有竞争性抑制人肝微粒体中甲苯妥英4-羟化酶活性的能力,Ki和Km值分别为559μM和235μM[4]。
• 体内研究: 苯苏西胺(腹腔注射；1.25 mmol/kg；单次剂量)可导致肾功能轻度变化,包括：微量血尿、蛋白尿增加和帕米诺马尿酸盐摄取减少[1]。苯苏肟(腹腔注射；0.3或0.6 mmol/kg；5-7天)会导致短暂性血尿和蛋白尿,但其他肾功能参数没有变化。结论是,苯苏肟对Fischer 344大鼠产生轻微的、短暂的肾脏作用,而Fischer 344大鼠是研究苯苏肟对泌尿道毒性的合适模型[1]。动物模型：Fischer 344大鼠[1]剂量：0.3或0.6mmol/kg给药：腹腔注射；5-7d结果：Fischer 344大鼠每日给药5-7d后出现尿毒性。
• 参考文献:

  [1]. G O Rankin, et al. Urinary Tract Effects of Phensuximide in the Sprague-Dawley and Fischer 344 Rat. J Appl Toxicol. . 1986 Oct;6(5):349-56.

  [2]. J A Ferrendelli, et al. Inhibitory Effects of Anticonvulsant Drugs on Cyclic Nucleotide Accumulation in Brain. Ann Neurol. 1979 Jun;5(6):533-8.

  [3]. J G MILLICHAP, et al. Milontin: A New Drug in the Treatment of Petit Mal.Lancet. 1952 Nov 8;2(6741):907-10.

  [4]. S D Hall,et al. Characterization and inhibition of mephenytoin 4-hydroxylase activity in human liver microsomes. The JOURNAL OP PHARMAcOLOGY AND EXPERIMENTAL THERAPEUTICS

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : WN3325000 CHEMICAL NAME : Succinimide, N-methyl-2-phenyl- CAS REGISTRY NUMBER : 86-34-0 BEILSTEIN REFERENCE NO. : 0155329 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C11-H11-N-O2 MOLECULAR WEIGHT : 189.23 WISWESSER LINE NOTATION : T5VNVTJ B1 DR HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 700 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 - mouse DOSE/DURATION : 485 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 : 795 mg/kg/7D-I TOXIC EFFECTS : Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - hematuria Kidney, Ureter, Bladder - inflammation, necrosis, or scarring of bladder TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 666 mg/kg SEX/DURATION : female 8-10 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - other developmental abnormalities TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported DOSE : 1533 mg/kg SEX/DURATION : female 8-10 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system MUTATION DATA TYPE OF TEST : Cytogenetic analysis TEST SYSTEM : Human Leukocyte DOSE/DURATION : 100 ug/L 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: 116,867,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4457 No. of Facilities: 46 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 279 (estimated) No. of Female Employees: 46 (estimated)

安全

• 危险品运输编码: NONH for all modes of transport
• 海关编码: 2925190090

合成路线

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海关

海关编码	2925190090
中文概述	2925190090 其他酰亚胺及其衍生物盐. 增值税率:17.0% 退税率:9.0% 监管条件:无 最惠国关税:6.5% 普通关税:30.0%
申报要素	品名, 成分含量, 用途
Summary	2925190090 other imides and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%