1001175-40-1Relevant academic research and scientific papers
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists
Betschmann, Patrick,Bettencourt, Brian,Donnelly-Roberts, Diana,Friedman, Michael,George, Jonathan,Hirst, Gavin,Josephsohn, Nathan,Konopacki, Donald,Li, Biqin,Maull, John,Morytko, Michael J.,Moore, Nigel StJohn,Namovic, Marian,Rafferty, Paul,Salmeron-Garcia, Jose-Andres,Tarcsa, Edit,Wang, Lu,Woller, Kevin
, p. 3848 - 3851 (2008)
A novel series of cyanoguanidine-piperazine P2X7 antagonists were identified and structure-activity relationship (SAR) studies described. Compounds were assayed for activity at human and rat P2X7 receptors in addition to their ability to inhibit IL-1β release from stimulated human whole blood cultures. Compound 27 possesses potent activity (0.12 μM) in this latter assay and demonstrates moderate clearance in-vivo.
