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恩前列素

恩前列素用途

为合成的去氢PGE2，能抑制动物和人体的基础胃酸和由组胺、五肽胃泌素、食物等引起的胃酸分泌。用于胃炎、胃溃疡及十二指肠溃疡。

恩前列素名称

[ CAS 号 ]:
73121-56-9

[ 中文名 ]:
恩前列素

[ 英文名 ]:
Enprostil

[中文别名 ]:

恩前列腺素

[英文别名 ]:

Enprostil (JAN/USAN/INN)
Syngard
Enprostil
Camleed (TN)
Gardrine
Camleed
Gardrin

恩前列素生物活性

[ 描述 ]:

恩前列素(RS 84135)是一种前列腺素E2衍生物。恩前列素能抑制阿莫胃泌素刺激的胃酸分泌,并能减少胃蛋白酶的分泌。Enprostil也可以作为抗溃疡剂,用于十二指肠或胃溃疡的研究[1][2]。

[ 相关类别 ]:

研究领域 >> 内分泌

信号通路 >> 其他 >> 其他

[参考文献]

[1]. Kohli Y, et al. Antisecretory effect of a PGE2 derivative, enprostil (TA/RS-84135): inhibitory action of amogastrin-stimulated secretion. Drugs Exp Clin Res. 1988;14(11):673-8.

[2]. Goa K L, et al. Enprostil: a preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of peptic ulcer disease[J]. Drugs, 1987, 34(5): 539-559.

恩前列素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
552.9±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₃H₂₈O₆

[ 分子量 ]:
400.46

[ 闪点 ]:
185.7±23.6 °C

[ 精确质量 ]:
400.188599

[ PSA ]:
93.06000

[ LogP ]:
1.45

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.586

恩前列素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MI5433000

CHEMICAL NAME :: 4,5-Heptadienoic acid, 7-(3-hydroxy-2-(3-hydroxy-4-phenoxy-1-butenyl)-5-oxoc yclopentyl)-, methyl ester, (1-alpha,2-beta(1E,3R*),3-alpha)-

CAS REGISTRY NUMBER :: 73121-56-9

LAST UPDATED :: 199504

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C23-H28-O6

MOLECULAR WEIGHT :: 400.51

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 :: >1600 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - cyanosis Musculoskeletal - other changes Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,2327,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >160 ug/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,2327,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,2327,1989

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 80 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,2327,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >320 ug/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 23,2327,1989

恩前列素合成路线

详细合成路线

恩前列素上下游产品

恩前列素上游产品

恩前列素下游产品

恩前列素制备

化合物(Ⅰ)先经硅烷化，再氧化，然后脱硅烷基，得到恩前列素。