1421-14-3

• 常用中文名：普尔安
• 常用英文名：Sombrevin
• CAS号：1421-14-3
• 分子式：C₁₈H₂₇NO₅
• 分子量：337.41100
• 相关类别： 原料药 Anesthetic Agents General anesthetics
• 发布时间：2018-09-14 17:07:59
• 更新时间：2024-01-12 00:56:14
• 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]。

名称

• 中文名: 丙泮尼地
• 英文名: propyl 2-[4-[2-(diethylamino)-2-oxoethoxy]-3-methoxyphenyl]acetate
• 中文别名: 普尔安
• 英文别名: Epontol; Sombrevin; Bayer 1420; Propantan; Fabontal; Fabantol; Propanidid; propanidide

物化性质

• 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

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。

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

安全

• 海关编码: 2924299090

合成路线

52744-26-0 2315-36-8 ~% 1421-14-3

文献：US2003/153554 A1, ;

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%