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普尔安

普尔安用途

丙胺(Sombrevin；Fabantol)是一种γ-氨基丁酸a型(GABAA)受体激动剂和一种短效非巴比妥类全身麻醉剂。丙胺可降低动脉压[1][2]。

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普尔安名称

[ CAS 号 ]:
1421-14-3

[ 中文名 ]:
丙泮尼地

[ 英文名 ]:
Sombrevin

[中文别名 ]:

普尔安

[英文别名 ]:

Epontol
Sombrevin
Bayer 1420
Propantan
Fabontal
Fabantol
Propanidid
propanidide

普尔安生物活性

[ 描述 ]:

丙胺(Sombrevin；Fabantol)是一种γ-氨基丁酸a型(GABAA)受体激动剂和一种短效非巴比妥类全身麻醉剂。丙胺可降低动脉压[1][2]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[ 靶点 ]

GABAA receptor[1]

[体内研究]

丙交酯(Sombrevin)(3-5 mg/kg；注入股静脉；单剂量)改变了58个视觉皮层神经元的定向调谐[3]。动物模型：成年猫(用D-tubocurarine固定)[3]剂量：3-5mg/kg给药：注入股静脉；单剂量结果：在58个初级视觉皮层神经元中,60%的神经元发生了47.6±5.6度的可靠定向变化,而在其余的细胞中,在麻醉的所有阶段,定向都是稳定的。55%的神经元的定向调谐宽度平均可靠地变化了65.2±6.7度,而31%的神经元调谐尖锐度更差,但24%的神经元更尖锐。优选的定向、调谐的宽度和神经元放电的频率通常在麻醉开始后30分钟内恢复。

普尔安物理化学性质

[ 密度 ]:
1.087g/cm3

[ 沸点 ]:
459.7ºC at 760mmHg

[ 分子式 ]:
C₁₈H₂₇NO₅

[ 分子量 ]:
337.41100

[ 闪点 ]:
231.8ºC

[ 精确质量 ]:
337.18900

[ PSA ]:
65.07000

[ LogP ]:
2.43810

[ 蒸汽压 ]:
1.24E-08mmHg at 25°C

[ 折射率 ]:
1.503

普尔安毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG9625000

CHEMICAL NAME :: Acetic acid, (4-((diethylcarbamoyl)methoxy)-3-methoxyphenyl)-, propyl ester

CAS REGISTRY NUMBER :: 1421-14-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C18-H27-N-O5

MOLECULAR WEIGHT :: 337.46

WISWESSER LINE NOTATION :: 3OV1R CO1 DO1VN2&2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Biochemical - Metabolism (Intermediary) - histamines (including liberation not immunochemical in origin)

REFERENCE :: BJANAD British Journal of Anesthesia. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1923- Volume(issue)/page/year: 45,1097,1973

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 81 mg/kg

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

REFERENCE :: AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 113 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: 19,845,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 80 mg/kg

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

REFERENCE :: AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 80 mg/kg

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

REFERENCE :: AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 75 mg/kg

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

REFERENCE :: AASXAP Acta Anaesthesiologica Scandinavica, Supplementum. (Munksgaard International Pub., POB 2148, DK-1016 Copenhagen K, Denmark) No.1- 1959- Volume(issue)/page/year: 17,21,1965 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 1200 mg/kg

SEX/DURATION :: female 1-60 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - physical

REFERENCE :: NYSJAM New York State Journal of Medicine. (Medical Soc. of the State of New York, POB 5405, Lake Success, NY 11042) V.1- 1901- Volume(issue)/page/year: 64,2177,1964

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普尔安安全信息

[ 海关编码 ]:
2924299090

普尔安合成路线

详细合成路线

普尔安海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 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, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

普尔安