Structure-Activity Relationship Studies on N'-Aryl Carbohydrazide P2X7 Antagonists.
作者
Nelson, Derek W.;Sarris, Kathy;Kalvin, Douglas M.;Namovic, Marian T.;Grayson, George;Donnelly-Roberts, Diana L.;Harris, Richard;Honore, Prisca;Jarvis, Michael F.;Faltynek, Connie R.;Carroll, William A.;
[摘要]：Structure-activity relationship (SAR) studies evaluated functional activity by monitoring calcium flux inhibition in cell lines expressing recombinant human and rat P2X7 receptors. Selected analogs were assayed in vitro for their capacity to inhibit release of cytokine IL-1b. Compds. with potent antagonist function were evaluated in vivo using effectively attenuated mech. allodynia in a rat model of neuropathic pain.
