| Identification | Back Directory | [Name]
N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-2,3-DIHYDRO-1,4-BENZODIOXIN-6-CARBOXAMIDE FUMARATE | [CAS]
527680-56-4 | [Synonyms]
PH-568487
PHA 568487
PHA 568487 free base
1,4-Benzodioxin-6-carboxamide, N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-2,3-dihydro-
N-(3R)-1-AZABICYCLO[2.2.2]OCT-3-YL-2,3-DIHYDRO-1,4-BENZODIOXIN-6-CARBOXAMIDE FUMARATE
macrophage,fracture,acetylcholine,Inhibitor,ischemic,bone,receptor,PHA 568487 free base,cerebral,middle,Post-stroke,stroke,inhibit,PHA568487,memory,oxidative,polarization,dysfunction,Nicotinic acetylcholine receptors,occlusion,PHA-568487,neuroinflammation,nicotinic,artery,stress,nAChR | [Molecular Formula]
C16H20N2O3 | [MDL Number]
MFCD11519961 | [MOL File]
527680-56-4.mol | [Molecular Weight]
288.34 |
| Hazard Information | Back Directory | [Uses]
PHA 568487 is an agonist of AChR α7. | [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.
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| 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.
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| [storage]
Desiccate at RT |
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