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利马前列素

利马前列素用途

Limaprost(OP1206)是PGE1类似物,是血小板粘附抑制剂。

利马前列素名称

[ CAS 号 ]:
74397-12-9

[ 中文名 ]:
利马前列素

[ 英文名 ]:
Limaprost

[中文别名 ]:

利马司特

[英文别名 ]:

17S,20-Dimethyl-trans-delta2-PGE1
Limaprost
17S,20-Dimethyl-trans-2,3-didehydro-PGE1
17S-Methyl-w-homo-trans-D2-PGE1
ONO 1206
OP 1206

利马前列素生物活性

[ 描述 ]:

Limaprost(OP1206)是PGE1类似物,是血小板粘附抑制剂。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> PGE合成酶

研究领域 >> 炎症/免疫

[参考文献]

[1]. Tsuboi, T., et al., Pharmacological evaluation of OP 1206, a prostaglandin E1 derivative, as an antianginal agent. Arch Int Pharmacodyn Ther, 1980. 247(1): p. 89-102.

[相关活性小分子]

利马前列素物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
550.6±50.0 °C at 760 mmHg

[ 熔点 ]:
97-100°

[ 分子式 ]:
C₂₂H₃₆O₅

[ 分子量 ]:
380.518

[ 闪点 ]:
300.9±26.6 °C

[ 精确质量 ]:
380.256287

[ PSA ]:
94.83000

[ LogP ]:
3.15

[ 外观性状 ]:
crystalline

[ 蒸汽压 ]:
0.0±3.4 mmHg at 25°C

[ 折射率 ]:
1.551

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
DMF: soluble

利马前列素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UK8362500

CHEMICAL NAME :: Prost-2,13-dien-1-oic acid, 11,15-dihydroxy-17,20-dimethyl-9-oxo-, (2E,11-alpha,13E,15S,17S)-

CAS REGISTRY NUMBER :: 74397-12-9

LAST UPDATED :: 199806

DATA ITEMS CITED :: 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

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

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2041368

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 12 mg/kg

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

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2041368

利马前列素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
UK8362500

利马前列素制备

88mg化合物(I)和357mg4-二甲氨基吡啶溶于二氯甲烷，在冰浴冷却下加入116脚甲磺酰氯。加毕，在30℃反应2.5h，得到94%的化合物(Ⅱ)。80mg化合物(Ⅱ)和800mg锌在含乙酸的异丙醇中，在50℃反应2h，得到66%的化合物(Ⅲ)。再酸性(如三氟乙酸或甲磺酸)水解为化合物(Ⅳ)，最后用猪肝酯酶水解，得到利马前列素。

利马前列素文献

OP-1206, a prostaglandin E1 derivative, attenuates the thermal hyperesthesia induced by constriction injury to the sciatic nerve in the rat.

Anesth. Analg. 80(3) , 515-20, (1995)

Nerve ischemia induces wallerian degeneration and peripheral neuropathy, the nerve constriction injury induces thermal hyperesthesia. Nerve ischemia is one possible mechanism in the development of the...

Inhibition of platelet aggregation by the cAMP-phosphodiesterase inhibitor, cilostamide, may not be associated with activation of cAMP-dependent protein kinase.

Cell. Signal. 4(4) , 453-63, (1992)

We examined the involvement of cAMP-dependent protein kinase (A kinase)2 in the inhibition by cilostamide, a specific inhibitor of the low Km cAMP-phosphodiesterase (PDE), on 9,11-epithio-11,12-methan...

Correlation between methotrexate-induced intestinal damage and decrease in polyamine content.

Life Sci. 72(6) , 669-76, (2002)

A synthetic analog of prostaglandin E(1), OP-1206 [17S, 20-dimethyl-trans-Delta(2)-prostaglandin E(1)] protects the small intestine from the methotrexate (MTX)-induced damage. The purpose of this stud...

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