527680-56-4

527680-56-4 structure

Name: PHA 568487
Chemical Name: N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide,but-2-enedioic acid
CAS Number: 527680-56-4
Molecular Formula: C₂₀H₂₄N₂O₇
Molecular Weight: 404.41400
Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
Create Date: 2016-06-01 22:41:51
Modify Date: 2024-01-12 15:13:06
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].

Name	N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide,but-2-enedioic acid

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR Signaling Pathways >> Neuronal Signaling >> nAChR Research Areas >> Neurological Disease
In Vitro	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: C57BL/6J male mice (10-12 weeks old) with pMCAO[2] 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[3] 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.
References	[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.

Molecular Formula	C₂₀H₂₄N₂O₇
Molecular Weight	404.41400
Exact Mass	404.15800
PSA	125.40000
LogP	1.32240

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