LimapROSt 是PGE1类似物,也是口服具有活性的血管舒张剂。它能够增加血流量以及减少血小板聚集。它具有抗心绞痛的功能,可用于疼痛的缓解,以及用于研究缺血性症状。
产品描述
Limaprost is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency.It is a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.
体外活性
By a concentration-dependent manner, Limaprost inhibits the IL-1-mediated induction of nerve growth factor (IC50: 70.9 ?nM human IVD cells) [3].
体内活性
PGE1 and limaprost exhibited a novel pharmacological action that suppresses NGF expression in human IVD cells, and other prostanoids differentially regulated NGF expression.?Limaprost has been used to treat patients with lumbar spinal stenosis in Japan and was proved to be effective in relieving symptoms.Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs are inhibited by oral administration of Limaprost at the same doses or doses less than those relieving vasopressin-induced ST depression of ECG.?Intra-coronary injection of Limaprost (1-100 ng/kg) in dogs causes a remarkable increase in coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption, and redox potential.?Limaprost given orally at more than 100 mg/kg relieves vasopressin-induced ST depression of rat electrocardiogram.?Resistance in both large and small vessels of the dog coronary artery is decreased by intravenous injection of Limaprost (1-3 mg/kg) [1].
Cas No.
74397-12-9
分子式
C22H36O5
分子量
380.52
别名
ONO1206;OP1206;利马前列素;17α,20-dimethyl-δ2-PGE1
储存和溶解度
DMSO:40 mg/mL (105.12 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years