Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432.

@article{Lord2014PharmacologyOA,
  title={Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432.},
  author={Brian Lord and Leah E Aluisio and James R. Shoblock and Robert A Neff and Elena I. Varlinskaya and Marc Ceusters and Timothy W. Lovenberg and Nicholas I. Carruthers and Pascal Bonaventure and Michael A Letavic and Terrence Deak and Wilhelmus H.I.M. Drinkenburg and Anindya Bhattacharya},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2014},
  volume={351 3},
  pages={628-41}
}
In the central nervous system, the ATP-gated Purinergic receptor P2X ligand-gated ion channel 7 (P2X7) is expressed in glial cells and modulates neurophysiology via release of gliotransmitters, including the proinflammatory cytokine interleukin (IL)-1β. In this study, we characterized JNJ-42253432 [2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide] as a centrally permeable (brain-to-plasma ratio of 1), high-affinity P2X7 antagonist with… CONTINUE READING
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