For research use only. Not for therapeutic Use.
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively[1].
When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED50 of 10 mg/kg for SERT occupancy[1].
| Catalog Number | I029829 |
| CAS Number | 1428327-35-8 |
| Synonyms | 2-methyl-N-[[1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl]-3,4-dihydro-1H-isoquinoline-5-carboxamide |
| Molecular Formula | C28H38N4O |
| Purity | ≥95% |
| InChI | InChI=1S/C28H38N4O/c1-30-16-13-25-23(21-30)9-8-12-26(25)27(33)29-22-28(14-6-3-7-15-28)32-19-17-31(18-20-32)24-10-4-2-5-11-24/h2,4-5,8-12H,3,6-7,13-22H2,1H3,(H,29,33) |
| InChIKey | DIKKTLPJDURHSW-UHFFFAOYSA-N |
| SMILES | CN1CCC2=C(C1)C=CC=C2C(=O)NCC3(CCCCC3)N4CCN(CC4)C5=CC=CC=C5 |
| Reference | [1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41. |
