PHA 568487

Product NamePHA 568487
CAS527680-57-5
MFC20H24N2O7
MW404.41376
EINECS
MOL File527680-57-5.mol

Chemical Properties

solubility	Soluble to 100 mM in water and to 100 mM in DMSO
form	Powder

Usage And Synthesis

Uses

PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR)[1][2].PHA 568487 reduces neuroinflammation and oxidative stress[2]. PHA-568487 has rapid brain penetration[3].

in vivo

PHA 568487 attenuates neuronal injury and behavioral dysfunction in mice with ischemic stroke only and ischemic stroke plus tibia fracture^[2].
PHA 568487 (1.25 mg/kg; i.p.; treated daily)-treated ischemic rats shows a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome^[4].

Animal Model:	C57BL/6J male mice (10-12 weeks old)^[2]
Dosage:	PHA 568487 (PHA; 0.4 and 0.8 mg/kg); Methyllycaconitine (MLA; 4 and 6 mg/kg)
Administration:	Injected intraperitoneally once on day 1, or twice on days 1 and 2, after pMCAO
Result:	Injection of PHA (0.8 mg/kg) and MLA (6 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 (297 6±8.3 g)^[4]
Dosage:	1.25 mg/kg
Administration:	I.p.;0.1 mL; treated daily
Result:	Showed a significant reduction of the cerebral infarct volumes and an improvement of the neurologic outcome.

storage

Desiccate at RT

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. PMID:20642449
[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. DOI:10.1111/jnc.12817
[3] Dingquan Zou,et al.Activation of Alpha-7 Nicotinic Acetylcholine Receptor Reduces Brain Edema in Mice with Ischemic Stroke and Bone Fracture. Mol Neurobiol.2017 Dec;54(10):8278-8286. DOI:10.1007/s12035-016-0310-8
[4] 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. DOI:10.1002/glia.23326

Preparation Products And Raw materials

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