依前列醇

依前列醇用途

为原发性肺动脉高血压治疗药。该品具有抗血小板和舒张血管作用，故可防止血栓形成。

依前列醇名称

[ CAS 号 ]:
35121-78-9

[ 中文名 ]:
依前列醇

[ 英文名 ]:
Epoprostenol

[中文别名 ]:

前列环素

[英文别名 ]:

PGX
Epoprostenol
MFCD00135629
Prostaglandin l2
prostacyclin
Vasocyclin
PGl2
ProstaglandinI
PGX(prostaglandin)
Cyclo-Prostin

依前列醇生物活性

[ 描述 ]:

依前列烯醇(前列腺素I2)是天然前列腺素衍生物前列环素(前列腺素I 2)的合成形式,在世界范围内注册用于治疗肺动脉高压(PAH)。依前列烯酚作为血小板聚集的有效抑制剂用于肺动脉高压和移植[1]。

[ 相关类别 ]:

研究领域 >> 心血管疾病

[ 靶点 ]

Human Endogenous Metabolite

[参考文献]

[1]. Provencher S, et al.Quality of life, safety and efficacy profile of thermostable flolan in pulmonary arterialhypertension. PLoS One. 2015 Mar 20;10(3):e0120657.

依前列醇物理化学性质

[ 密度 ]:
1.221g/cm3

[ 沸点 ]:
530.2ºC at 760mmHg

[ 分子式 ]:
C₂₀H₃₁NaO₅

[ 分子量 ]:
374.44700

[ 闪点 ]:
182.1ºC

[ 精确质量 ]:
374.20700

[ PSA ]:
89.82000

[ LogP ]:
2.07380

[ 折射率 ]:
1.611

依前列醇毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UK8008500

CHEMICAL NAME :: Prosta-5,13-dien-1-oic acid, 6,9-epoxy-11,15-dihydroxy-, (5Z,9-alpha,11-alpha,13E,15S)-

CAS REGISTRY NUMBER :: 35121-78-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C20-H32-O5

MOLECULAR WEIGHT :: 352.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 mg/kg

SEX/DURATION :: female 15-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: GOBIDS Gynecologic and Obstetric Investigation. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.9- 1978- Volume(issue)/page/year: 33,193,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 800 ng/kg

SEX/DURATION :: female 1-4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Maternal Effects - other effects

REFERENCE :: JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 94,279,1992

依前列醇安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S22;S26;S36

依前列醇合成路线

详细合成路线

依前列醇制备

9,11,15-三羟基前列-5,13-二烯-1-酸经醚化，再和N-溴代丁二酰亚胺于四氢呋喃-氯仿的混合溶剂中反应，产品经水解，消除溴化氢，得到依前列醇。