产品
编 号:F380022
分子式:C16H20N2O3
分子量:288.34
产品类型
结构图
CAS No: 527680-56-4
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产品详情
生物活性:
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation.
体内研究:
PHA 568487 treatment reduces mouse cognitive decline caused by aseptic bone fracture by promoting inflammation resolution. PHA 568487 (PHA; 0.8 mg/kg; injected intraperitoneally) reduces infarct volume and TUNEL positive neurons in the peri-infarct regions of permanent middle cerebral artery occlusion (pMCAO) and pMCAO+tibia fracture mice.The role played by a7 receptors on neuroinflammation is supported by the decrease of [18F]DPA-714 binding in ischemic rats treated with the a7 agonist PHA 568487 at day 7 after MCAO. PHA 568487-treated ischemic rats show a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome compared with non-treated MCAO rats.Animal Model:C57BL/6J male mice (10-12 weeks old) with pMCAO
Dosage:0.4 and 0.8 mg/kg
Administration:Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result:0.8 mg/kg on days 1 and 2 after pMCAO yielded the best effect on infarct volume and behavior tests.
Animal Model:Adult male Sprague-Dawley rats
Dosage:1.25 mg/kg
Administration:Treated i.p. daily with 0.1 mL
Result:Showed a significant decrease of [18F]DPA-714 binding in the ischemic cerebral hemisphere in comparison to non-treated ischemic rats.
体外研究:
PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells.PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia.