盐酸奥普力农
| 中文名称 | 盐酸奥普力农 |
|---|---|
| 中文同义词 | 1,2-二氢-5-咪唑并[...;盐酸奥普力农;化合物 T5033L |
| 英文名称 | OLPRINONE HYDROCHLORIDE |
| 英文同义词 | 3-pyridinecarbonitrile,1,2-dihydro-5-(imidazo(1,2-a)pyridin-6-yl)-6-methyl-2-o;e1020;xo-,monohydrochloride,monohydrate;OLPRINONE HCL;1,2-Dihydro-5-imidazo[1,2-α]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile Hydrochloride;Coretec;Loprinone hydrochloride, 1,2-Dihydro-5-(imidazo[1,2-a]pyridin-6-yl)-6-methyl-2-oxo-3-pyridinecarbonitrile hydrochloride;3-Pyridinecarbonitrile,1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-,monohydrochloride |
| CAS号 | 119615-63-3 |
| 分子式 | C14H11ClN4O |
| 分子量 | 286.72 |
| EINECS号 | |
| 相关类别 | 对照品;Heterocyclic Compounds;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 119615-63-3.mol |
| 结构式 |  |
盐酸奥普力农 性质
| 熔点 | >3000C |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≤4 毫克/毫升 |
| 形态 | 固体 |
| 颜色 | 米色 |
Olprinone (Loprinone) Hydrochloride 是一种有效的磷酸二酯酶 (PDE) 3 抑制剂，对 PDE1，PDE2，PDE3，PDE4 的 IC50 分别为 150、100、0.35 和 14 μM。Olprinone Hydrochloride 因其正性肌力和血管扩张作用而被用于心力衰竭的研究。Olprinone Hydrochloride 具有抗炎活性。
Olprinone (Loprinone) Hydrochloride (0.2 mg/kg; i.p.) modulates the inflammation associated with myocardial ischemia-reperfusion injury in rats.
| Animal Model: | Male adult Wistar rats (250-300 g) (ischemia–reperfusion rats) |
| Dosage: | 0.2 mg/kg |
| Administration: | I.p. (administered 15 min after ischemia) |
| Result: | Significantly reduced the: (1) histological evidence of myocardial injury, (2) pro-inflammatory cytokines: tumor necrosis factor-α (TNF-α) and Interleukin-1β (IL-1β), (3) adhesion molecules: Inter-Cellular Adhesion Molecule 1 (ICAM-1) and P-Selectin, (4) nitrotyrosine formation, (5) nuclear factor kappa-B (NF-κB) expression, (6) Poly (ADP-ribose) (PAR) formation, and (7) apoptosis (Bax, Bcl-2, Fas-L and terminal deoxynucleotidyl transferase-mediated UTP end labeling (TUNEL). |