苯琥胺

苯琥胺用途

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。

苯琥胺名称

[ CAS 号 ]:
86-34-0

[ 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

苯琥胺生物活性

[ 描述 ]:

[ 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

苯琥胺物理化学性质

[ 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

苯琥胺毒性和生态

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)

苯琥胺安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2925190090

苯琥胺合成路线

详细合成路线

苯琥胺上下游产品

苯琥胺上游产品

苯琥胺下游产品

苯琥胺海关

[ 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%

苯琥胺