| Bioactivity | PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation[1][2][3]. | ||||||||||||
| Invitro | PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells[2].PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia[3]. | ||||||||||||
| In Vivo | 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[2].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[3]. 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[3]. Animal Model: | ||||||||||||
| Name | PHA 568487 free base | ||||||||||||
| CAS | 527680-56-4 | ||||||||||||
| Formula | C16H20N2O3 | ||||||||||||
| Molar Mass | 288.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. F Barclay Shilliday, et al. Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. Drug Metab Lett. 2010 Aug;4(3):162-72. [2]. Zhenying Han, et al. Alpha-7 nicotinic acetylcholine receptor agonist treatment reduces neuroinflammation, oxidative stress, and brain injury in mice with ischemic stroke and bone fracture. J Neurochem. 2014 Nov;131(4):498-508. [3]. Lorena Colás, et al. In vivo imaging of Α7 nicotinic receptors as a novel method to monitor neuroinflammation after cerebral ischemia. Glia. 2018 Aug;66(8):1611-1624. |
PHA 568487 free base
CAS: 527680-56-4 F: C16H20N2O3 W: 288.34
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base
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