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丙泊酚

丙泊酚用途

Propofol 有效直接地激活 GABAA 受体和抑制谷氨酸受体介导的兴奋性突触传递。Propofol 具有抗伤害感受特性,可用于镇静和催眠。

丙泊酚名称

[ CAS 号 ]:
2078-54-8

[ 中文名 ]:
2,6-二异丙基苯酚

[ 英文名 ]:
Propofol

[中文别名 ]:

[英文别名 ]:

2,6-i-Pr2-C6H3-OH
Diisopropylphenol
2,6-di-iso-Propylphenol
2,6-di(propan-2-yl)phenol
Propofolum
Disoprofol
2-hydroxy-1,3-diisopropylbenzene
Fresofol
Diprivan
EINECS 218-206-6

丙泊酚生物活性

[ 描述 ]:

Propofol 有效直接地激活 GABAA 受体和抑制谷氨酸受体介导的兴奋性突触传递。Propofol 具有抗伤害感受特性,可用于镇静和催眠。

[ 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[1]

[体内研究]

异丙酚(i.p.；40 mg/kg)引起的镇静完全恢复发生在36.3分钟。ECT评估时有残留的抗伤害作用,但用毒热评估时没有。

[参考文献]

[1]. R Nadeson, et al. Antinociceptive Properties of Propofol: Involvement of Spinal Cord Gamma-Aminobutyric acid(A) Receptors. J Pharmacol Exp Ther . 1997 Sep;282(3):1181-6.

丙泊酚物理化学性质

[ 密度 ]:
0.9±0.1 g/cm3

[ 沸点 ]:
256.0±0.0 °C at 760 mmHg

[ 熔点 ]:
18 °C(lit.)

[ 分子式 ]:
C₁₂H₁₈O

[ 分子量 ]:
178.271

[ 闪点 ]:
107.5±7.2 °C

[ 精确质量 ]:
178.135757

[ PSA ]:
20.23000

[ LogP ]:
4.16

[ 外观性状 ]:
淡黄色液体

[ 蒸汽压 ]:
0.0±0.5 mmHg at 25°C

[ 折射率 ]:
1.513

[ 储存条件 ]:
0-6°C

丙泊酚MSDS

丙泊酚毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SL0810000

CHEMICAL NAME :: Phenol, 2,6-diisopropyl-

CAS REGISTRY NUMBER :: 2078-54-8

BEILSTEIN REFERENCE NO. :: 1866484

LAST UPDATED :: 199710

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C12-H18-O

MOLECULAR WEIGHT :: 178.30

WISWESSER LINE NOTATION :: QR BY1&1 FY1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 386 mg/kg/14D-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - pleural thickening

REFERENCE :: CCMDC7 Critical Care Medicine. (Williams & Wilkins, 428 E. Preston Street, Baltimore, MD 21202) V.1- 1973- Volume(issue)/page/year: 23,1928,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 2857 ug/kg/1D-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - rigidity (including catalepsy) Behavioral - irritability

REFERENCE :: ANASAB Anaesthesia. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1946- Volume(issue)/page/year: 43,170,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 500 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,953,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 42 mg/kg

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

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 21,11,1993

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1100 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,953,1995

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 170 mg/kg

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

REFERENCE :: JMPCAS Journal of Medicinal and Pharmaceutical Chemistry. (Washington, DC) V.1-5, 1959-62. For publisher information, see JMCMAR. Volume(issue)/page/year: 2,201,1960

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - altered sleep time (including change in righting reflex) Behavioral - analgesia

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: 23,1350,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - sleep Behavioral - muscle weakness

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: 23,1350,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 2800 ug/kg

SEX/DURATION :: female 39 week(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - Apgar score (human only) Reproductive - Effects on Newborn - other neonatal measures or effects Reproductive - Effects on Newborn - behavioral

REFERENCE :: BJANAD British Journal of Anesthesia. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1923- Volume(issue)/page/year: 62,649,1989

丙泊酚安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S37/39

[ 危险品运输编码 ]:
2810

[ WGK德国 ]:
3

[ RTECS号 ]:
SL0810000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2907199090

丙泊酚合成路线

丙泊酚上下游产品

丙泊酚上游产品

丙泊酚下游产品

丙泊酚制备

1.丙烯与苯酚经烷基化而得。在强烈搅拌并充入氮气的情况下，将4.5g铝屑加入565g预热到165℃的苯酚中，待放出氢气后即可停止反应。将此反应混合物装入高压釜内，通入丙烯，在240℃反应2h。在反应过程中将压力从1.37MPa渐渐增加到3.43MPa。反应毕，冷却，将釜内物料加至200ml5%的盐酸中，震荡。将混合物过滤，水洗。加甲苯通过恒沸蒸馏干燥产物，再经分馏得到656g产品，收率61%

2.以异丁烯为原料，在三苯氧基铝催化下，对苯酚进行烷基化反应，可得丙泊酚。

丙泊酚海关

[ 海关编码 ]: 2907199090

[ 中文概述 ]:
2907199090 其他一元酚. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:5.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2907199090 other monophenols VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:5.5% General tariff:30.0%

丙泊酚文献

Ca(2+) permeation and/or binding to CaV1.1 fine-tunes skeletal muscle Ca(2+) signaling to sustain muscle function.

Skelet. Muscle 5 , 4, (2015)

Ca(2+) influx through CaV1.1 is not required for skeletal muscle excitation-contraction coupling, but whether Ca(2+) permeation through CaV1.1 during sustained muscle activity plays a functional role ...

Propofol increases morbidity and mortality in a rat model of sepsis.

Crit. Care 19 , 45, (2015)

Severe sepsis is associated with approximately 50% mortality and accounts for tremendous healthcare costs. Most patients require ventilatory support and propofol is commonly used to sedate mechanicall...

Propofol ameliorates calpain-induced collapsin response mediator protein-2 proteolysis in traumatic brain injury in rats.

Chin. Med. J. 128(7) , 919-27, (2015)

Collapsin response mediator protein-2 (CRMP2), a multifunctional cytosolic protein highly expressed in the brain, is degraded by calpain following traumatic brain injury (TBI), possibly inhibiting pos...

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丙泊酚