ARTICLE | Distillery Therapeutics

Therapeutics: Purinergic receptor P2X ligand-gated ion channel 7 (P2RX7; P2X7)

February 12, 2015 8:00 AM UTC

In vitro and rodent studies suggest 2,5-dioxoimidazolidine-based P2RX7 antagonists could help treat inflammatory disease and pain. Chemical synthesis of analogs of a research-use 2,5-dioxoimidazolidine antagonist of P2RX7 followed by testing in a cell-based P2RX7 activity assay identified several lead compounds that decreased two markers of P2RX7 activity by 3- to 10-fold compared with the parent compound. In mouse models of inflammatory pain and RA, one of the lead compounds decreased edema volume and the severity of RA pathology, respectively, compared with vehicle. Next steps could include testing the analogs in additional disease models. ...