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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.
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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 |
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