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

  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},
  volume={351 3},
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
Related Discussions
This paper has been referenced on Twitter 1 time. VIEW TWEETS


Publications citing this paper.
Showing 1-10 of 14 extracted citations


Publications referenced by this paper.
Showing 1-10 of 48 references

The role of purinergic signaling in depressive disorders.

Neuropsychopharmacologia Hungarica : a Magyar Pszichofarmakologiai Egyesulet lapja = official journal of the Hungarian Association of Psychopharmacology • 2012
View 4 Excerpts
Highly Influenced

Role of P2X7 ion channel in mood disorders: characterization of a P2X7 antagonist JNJ-42253432 in the rat

AAL Bhattacharya, J Shoblock, +7 authors T Lovenberg
brain, in Proceedings of the 29th CINPWorld Congress of Neuropsychopharmacology; • 2014
View 1 Excerpt

Similar Papers

Loading similar papers…