Cas No.: | 1428327-35-8 |
Chemical Name: | 2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide |
Synonyms: | JNJ 42253432;JNJ42253432 |
Formula: | C28H38N4O |
M.Wt: | 446.639 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |