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Chemical Structure : JNJ-42253432
Catalog No.: PC-60767Not For Human Use, Lab Use Only.
A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.
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A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively; does not block calcium flux via human P2X1, P2X2, P2X3, P2X2/P2X3, and P2X4 at 10 uM; attenuates both ATP- and Bz-ATP-induced currents from hP2X7-1321N1 cells with similar potencies (pEC50=7.0), blocks the release of IL-1β induced by Bz-ATP in freely moving rat brain, also increases serotonin levels; attenuates amphetamine-induced hyperactivity in vivo.
| M.Wt | 446.639 | |
| Formula | C28H38N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lord B, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
2. Amhaoul H, et al. Neuropharmacology. 2016 Jun;105:175-185.
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