PHA 568487

Research use only, not for human use.

The quinuclidine PHA 568487 is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

The quinuclidine PHA 568487 is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

PHA 568487, α-7 nAchR-specific agonist, prevents NF-κb activation in the cells.PHA 568487 treatment significantly reduces the expression of leukocyte infiltration molecules in MCAO rats and in endothelial cells after in vitro ischemia.

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.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. 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. Animal Model:C57BL/6J male mice (10-12 weeks old) with pMCAO 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 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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Endocrinology/Hormones

AChR

α7 nicotinic acetylcholine receptor

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527680-56-4

288.34

C16H20N2O3

>98% (HPLC)

H2O:<40.44mg/ml (100mM); DMSO:<40.44mg/ml (100mM)

O=C(c(cc1)cc2c1OCCO2)N[C@@H]1C(CC2)CCN2C1

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(-20℃)

With Ice Pack

≥ 2 years