- 英文名称
- Limaprost
- 分子式
- C22H36O5
- 分子量
- 380.52
- 中文别名
- 利马前列; 利马司特; 立马前列素; (2E,11α,13E,15S,17S)-11,15-二羟基-17,20-二甲基-9-氧代前列-2,13-二烯-1-酸; (E)-7-((1R,2R,3R)-3-羟基-2-((3S,5S,E)-3-羟基-5-甲基壬-1-烯-1-基)-5-氧代环戊基)庚-2-烯酸; Opalmon; Opaprosmon; Optiran; (2E)-7-{(1R,2R,3R)-3-hydroxy-2-[(1E,3S,5S)-3-hydroxy-5-methyl-1-nonenyl]-5-oxocyclopentyl}-2-heptenoic acid; 17S,20-Dimethyl-trans-D2-PGE1; Prorenal; Zeflopto; (2e,11-alpha,13e,15s,17s)-11,15-dihydroxy-17,20-dimethyl-9-oxoprost-2,13-die; 11α,15s-dihydroxy-17s,20-dimethyl-9-oxo-prosta-2e,13e-dien-1-oic acid; 2-Heptenoic acid, 7-[(1R,2R,3R)-3-hydroxy-2-[(1E,3S,5S)-3-hydroxy-5-methyl-1-nonenyl]-5-oxocyclopentyl]-, (2E)- (9CI); Prosta-2,13-dien-1-oic acid, 11,15-dihydroxy-17,20-dimethyl-9-oxo-, (2E,11a,13E,15S,17S)-; 17α,20-dimethyl-δ2-PGE1, 11α,15S-Dihydroxy-17S,20-dimethyl-9-oxo-prosta-2E,13E-dien-1-oic acid; (2E)-7-[(1R)-2β-[(1E,3S,5S)-3-Hydroxy-5-methyl-1-nonenyl]-3α-hydroxy-5-oxocyclopentan-1α-yl]-2-heptenoic acid
- 用途
- - 生物活性
Limaprost (OP1206) 是一种 PGE1 类似物，也是一种有效的口服活性血管舒张剂。Limaprost 可增加血流量并抑制血小板聚集。Limaprost 可用于缓解疼痛，具有抗心绞痛作用，并可用于缺血性症状的研究。
- 体外研究
Limaprost inhibits the IL-1-mediated induction of nerve growth factor (NGF) in a concentration-dependent manner with an IC
50
value of 70.9 nM human IVD cells.
- 体内研究
Limaprost (OP1206) given orally at more than 100 mg/kg relieves Argipressin-induced ST depression of rat electrocardiogram (ECG).
Intra-coronary injection of Limaprost (OP1206; 1-100 ng/kg) in dogs results in a remarkable increase of coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption and redox potential.
Resistance in both large and small vessels of dog coronary artery is decreased by intravenous injection of Limaprost (OP1206; 1-3 mg/kg).
Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs are inhibited by oral administration of Limaprost (OP1206) at the same doses or doses less than those relieving Argipressin-induced ST depression of ECG.
- 化学性质
白色结晶，熔点97～100℃。
- 对末梢循环有改善作用，对血小板的环磷酸苷含量，对血栓素的生成有抑制作用。用于闭塞性血栓血管炎及并发溃疡、疼痛及冷感等缺血症状。
