Limaprost

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

利马前列素是 PGE1 的类似物，经过结构修饰，旨在延长其半衰期并增强效力。它是一种有效的口服活性血管扩张剂。利马前列素增加血流量并抑制血小板聚集。利马前列素可用于缓解疼痛，具有抗心绞痛作用，并具有治疗缺血症状的潜力。

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.By a concentration-dependent manner, Limaprost inhibits the IL-1-mediated induction of nerve growth factor (IC50: 70.9 ?nM human IVD cells) [3].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).(In Vitro):Limaprost inhibits the IL-1-mediated induction of nerve growth factor (NGF) in a concentration-dependent manner with an IC50 value of 70.9 ?nM human IVD cells.(In Vivo):Limaprost (OP1206) given orally at more than 100 μg/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.

Limaprost inhibits the IL-1-mediated induction of nerve growth factor (NGF) in a concentration-dependent manner with an IC50 value of 70.9 ?nMhuman IVD cells.

Limaprost (OP1206) given orally at more than 100 μg/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.

17α,20-dimethyl-δ2-PGE1,ONO1206,OP1206

Immunology/Inflammation

PGE synthase

PGE Synthase

nervous system

Neurologic Claudication in Patients With Lumbar Spinal Stenosis

74397-12-9

380.52

C22H36O5

>98% (HPLC)

DMSO:40 mg/mL (105.12 mM)

O=C(O)/C=C/CCCC[C@@H]1[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)CC1=O

——

(-20℃)

With Ice Pack

≥ 2 years