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丙戊酰脲

丙戊酰脲用途

Apronal (Allylisopropylacetylurea, Apronalide) 是一种催眠和镇静药物,由于副作用已被一些国家撤市。

丙戊酰脲名称

[ CAS 号 ]:
528-92-7

[ 中文名 ]:
烯丙基异丙基乙酸脲

[ 英文名 ]:
Apronal

[中文别名 ]:

[英文别名 ]:

APRONALIDE
Allylisopropylacetylurea
Sedormid
Allylisopropylacetylcarbamide
Isopropylallylessigsaeure-ureid
(2-Isopropyl-4-pentenoyl)urea
2-Isopropyl-pent-4-ensaeure-ureid
Allylisoprorylacetylurea
EINECS 208-443-3
Apronal

丙戊酰脲生物活性

[ 描述 ]:

Apronal (Allylisopropylacetylurea, Apronalide) 是一种催眠和镇静药物,由于副作用已被一些国家撤市。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体内研究]

研究表明,烯丙基异丙基乙酰脲不仅增加了动物肝脏和尿液中卟啉的含量,而且还带来了明显的肝脏绿色色素沉着。用高剂量的烯丙基异丙基乙酰脲长期治疗大鼠恢复良好,并恢复到测量参数的正常值。通过长期给予烯丙基异丙基乙酰脲引起的病变可以被大鼠耐受并且是可逆的[1]。由于apronal报道固定药疹和粘膜皮肤眼综合征[2]。

[动物实验]

大鼠：将Apronal给予雄性Sandoz OFA-SPF大鼠，体重140-150g，每天两次相等的皮下注射，间隔8小时。总日剂量为400mg / kg，并且持续给药21天。对照大鼠类似地仅用丙二醇处理。将尿液样品收集在玻璃管中，固体CO2，温度并冷冻保存直至分析[1]。

[参考文献]

[1]. Rentsch G, et al. The effect of prolonged administration of allylisopropylacetylurea to rats on cytochrome P-450 and other liver haemoproteins. Xenobiotica. 1976 Mar;6(3):151-7.

[2]. Fujimoto Y, et al. Fixed drug eruption due to allylisopropylacetylurea. Contact Dermatitis. 1993 May;28(5):282-4.

[相关活性小分子]

丙戊酰脲物理化学性质

[ 密度 ]:
1.025g/cm3

[ 熔点 ]:
196 °C

[ 分子式 ]:
C₉H₁₆N₂O₂

[ 分子量 ]:
184.23600

[ 精确质量 ]:
184.12100

[ PSA ]:
72.19000

[ LogP ]:
2.12080

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.474

[ 储存条件 ]:
室温，干燥

[ 水溶解性 ]:
水溶性：可溶；可溶于：乙醚,醇

丙戊酰脲毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YT5775000

CHEMICAL NAME :: Urea, (2-isopropyl-4-pentenoyl)-

CAS REGISTRY NUMBER :: 528-92-7

BEILSTEIN REFERENCE NO. :: 1775529

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C9-H16-N2-O2

MOLECULAR WEIGHT :: 184.27

WISWESSER LINE NOTATION :: ZVMVY2U1&Y1&1

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 :: 1050 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JPHAA3 Journal of the American Pharmaceutical Association. (Washington, DC) V.1-28, 1912-39; New series: V.1-17, 1961-77. Volume(issue)/page/year: 23,788,1934

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1220 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DMWOAX Deutsche Medizinische Wochenschrift. (Stuttgart, Fed. Rep. Ger.) V.1-104, 1875-1979. Volume(issue)/page/year: 54,1166,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DMWOAX Deutsche Medizinische Wochenschrift. (Stuttgart, Fed. Rep. Ger.) V.1-104, 1875-1979. Volume(issue)/page/year: 54,1166,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DMWOAX Deutsche Medizinische Wochenschrift. (Stuttgart, Fed. Rep. Ger.) V.1-104, 1875-1979. Volume(issue)/page/year: 54,1166,1928

丙戊酰脲安全信息

[ 海关编码 ]:
2924210090

丙戊酰脲合成路线

详细合成路线

丙戊酰脲海关

[ 海关编码 ]: 2924210090

[ 中文概述 ]:
2924210090 其他酰脲及其衍生物以及它们的盐。监管条件:无。增值税率:17.0%。退税率:9.0%。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, 包装

[ Summary ]:
2924210090 other ureines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%