Name | PHA-568487 fumarate |
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Synonyms | (S)-Methylisothiourea sulfate |
Description | 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]. |
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Related Catalog | |
In Vitro | PHA 568487 increases anti-oxidant gene expression and decreases oxidative stress and phosphorylation of NF-κb p65. Methyllycaconitine (MLA) has the opposite effects[2]. PHA increases anti-oxidant genes and NADPH oxidase expression associated with decreased phosphorylation of NF-kB p65 in microglia/macrophages[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. |
References |
Molecular Formula | C20H24N2O7 |
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Molecular Weight | 404.41400 |
Exact Mass | 404.15800 |
PSA | 125.40000 |
LogP | 1.32240 |
Storage condition | -20°C |