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对氨基苯甲酸乙酯

对氨基苯甲酸乙酯用途

Benzocaine 与所有其它局部麻醉药 (LAs) 一起,作用电压门控Na+通道的共同受体,其在 +30 mV 下测得的 IC50 值为0.8 mM。

对氨基苯甲酸乙酯名称

[ CAS 号 ]:
94-09-7

[ 中文名 ]:
4-氨基苯甲酸乙酯

[ 英文名 ]:
Benzocaine

[中文别名 ]:

[英文别名 ]:

ORTHESIN
Americaine
Ora-jel
ethyl 4-aminobenzene carboxylate
Anaesthesin
AETHOFORM
Benzocainum
Ethyl 4-aminobenzoate
ethyl ester of p-aminobenzoic acid
Benzocaine

对氨基苯甲酸乙酯生物活性

[ 描述 ]:

Benzocaine 与所有其它局部麻醉药 (LAs) 一起,作用电压门控Na+通道的共同受体,其在 +30 mV 下测得的 IC50 值为0.8 mM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 0.8 mM (Na+ channel)[1].

[体外研究]

苯佐卡因以剂量依赖性方式阻断μ1野生型Na +电流。当施加+ 30mV的测试电位时,估计抑制50％Na +电流的苯佐卡因浓度(IC50)为约0.8mM。苯并卡因(从6.6到9.9 mV)也显着降低了h∞曲线的斜率。 μ1-N1584A的突变也显着增加了苯佐卡因的效力。在1mM时,苯佐卡因阻断约55％的野生型Na +电流但约95％的μ1-N1584A突变电流。与野生型相比,苯佐卡因似乎与N1584A突变体中的LA受体结合更强[1]。 Caz +摄取的抑制发生在较低的苯佐卡因浓度(IC50 = 40.3±1.2mM),而不是影响酶活性[2]。

[体内研究]

一种常见的含苯佐卡因麻醉剂局部应用于以下物种：狗,家养短毛猫,Long-Evans大鼠,Sprague-Dawley大鼠,雪貂,恒河猴,食蟹猴,猫头鹰猴,新西兰白兔,小型猪,ICR小鼠,C3H小鼠和C57BL/10SnJ小鼠。除小鼠和大鼠外,所有动物均接受2秒喷雾至鼻咽粘膜,估计剂量为56mg。对啮齿动物的口腔粘膜进行2秒喷雾可为这些动物提供过大量的液体。几个月后在狗中重复该研究以确认低反应。在大多数测试的动物中观察到对苯佐卡因喷雾的反应,在给药后15至30分钟内反应达到峰值[3]。

[参考文献]

[1]. Wang GK et al. A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels. Pflugers Arch. 1998 Jan;435(2):293-302.

[2]. Di Croce D et al. Drug action of benzocaine on the sarcoplasmic reticulum Ca-ATPase from fast-twitch skeletal muscle. Naunyn Schmiedebergs Arch Pharmacol. 2015 Nov;388(11):1163-70.

[3]. Davis JA, et al. Benzocaine-induced methemoglobinemia attributed to topical application of the anesthetic in several laboratory animal species. Am J Vet Res. 1993 Aug;54(8):1322-6.

[相关活性小分子]

对氨基苯甲酸乙酯物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
310.7±15.0 °C at 760 mmHg

[ 熔点 ]:
88-90 °C

[ 分子式 ]:
C₉H₁₁NO₂

[ 分子量 ]:
165.189

[ 闪点 ]:
164.2±17.9 °C

[ 精确质量 ]:
165.078979

[ PSA ]:
52.32000

[ LogP ]:
1.95

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±0.7 mmHg at 25°C

[ 折射率 ]:
1.555

[ 储存条件 ]:
0-6°C

[ 稳定性 ]:
Stable. Combustible. Incompatible with strong oxidizing agents.

对氨基苯甲酸乙酯MSDS

详细MSDS(安全技术说明书)

对氨基苯甲酸乙酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DG2450000

CHEMICAL NAME :: Benzoic acid, p-amino-, ethyl ester

CAS REGISTRY NUMBER :: 94-09-7

BEILSTEIN REFERENCE NO. :: 0638434

LAST UPDATED :: 199706

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C9-H11-N-O2

MOLECULAR WEIGHT :: 165.21

WISWESSER LINE NOTATION :: ZR DVO2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - guinea pig

REFERENCE :: JSCCA5 Journal of the Society of Cosmetic Chemists. (Soc. of Cosmetic Chemists, 1995 Broadway, Suite 1701, New York, NY 10023) V.1- 1947- Volume(issue)/page/year: 28,357,1977 ** ACUTE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Rectal

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 12 mg/kg

TOXIC EFFECTS :: Blood - methemoglobinemia-carboxyhemoglobin

REFERENCE :: NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 263,454,1960

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3042 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: TOVEFN Toksikologicheskii Vestnik. (18-20 Vadkovskii per. Moscow, 101479, Russia) History Unknown Volume(issue)/page/year: (2),34,1996

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2500 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: TOVEFN Toksikologicheskii Vestnik. (18-20 Vadkovskii per. Moscow, 101479, Russia) History Unknown Volume(issue)/page/year: (2),34,1996

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 216 mg/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 17,900,1974

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1150 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,33,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Bird - wild bird species

DOSE/DURATION :: 56 mg/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: 21,315,1972 *** REVIEWS *** TOXICOLOGY REVIEW PHREA7 Physiological Reviews. (American Physiological Soc., 9650 Rockville Pike, Bethesda, MD 20814) V.1- 1921- Volume(issue)/page/year: 12,190,1932 *** U.S. STANDARDS AND REGULATIONS *** EPA FIFRA 1988 PESTICIDE SUBJECT TO REGISTRATION OR RE-REGISTRATION FEREAC Federal Register. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) V.1- 1936- Volume(issue)/page/year: 54,7740,1989 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81723 No. of Facilities: 293 (estimated) No. of Industries: 8 No. of Occupations: 7 No. of Employees: 2005 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81723 No. of Facilities: 1499 (estimated) No. of Industries: 12 No. of Occupations: 17 No. of Employees: 167623 (estimated) No. of Female Employees: 146838 (estimated)

对氨基苯甲酸乙酯安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi:Irritant

[ 风险声明 (欧洲) ]:
R36/37/38;R43

[ 安全声明 (欧洲) ]:
22-24/25-37/39-26-24

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

[ WGK德国 ]:
2

[ RTECS号 ]:
DG2450000

[ 包装等级 ]:
III

[ 海关编码 ]:
2922499990

对氨基苯甲酸乙酯合成路线

详细合成路线

对氨基苯甲酸乙酯上下游产品

对氨基苯甲酸乙酯上游产品

对氨基苯甲酸乙酯下游产品

对氨基苯甲酸乙酯制备

1.主要采用酯化法。先由对硝基浓甲酸经加氢还原生成对氨基苯甲酸，然后在硫酸催化剂存在下与乙醇进行酯化反应，再经中和、洗涤、结晶、干燥而得。

对氨基苯甲酸乙酯海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 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, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

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