| Title : Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists - Nelson_2008_J.Med.Chem_51_3030 |
| Author(s) : Nelson DW , Sarris K , Kalvin DM , Namovic MT , Grayson G , Donnelly-Roberts D , Harris R , Honore P , Jarvis MF , Faltynek CR , Carroll WA |
| Ref : Journal of Medicinal Chemistry , 51 :3030 , 2008 |
|
Abstract :
N'-aryl acyl hydrazides were identified as P2X7 receptor antagonists. 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-1beta. Compounds with potent antagonist function were evaluated in vivo using the zymosan-induced peritonitis model. A representative compound effectively attenuated mechanical allodynia in a rat model of neuropathic pain. |
| PubMedSearch : Nelson_2008_J.Med.Chem_51_3030 |
| PubMedID: 18438986 |
Nelson DW, Sarris K, Kalvin DM, Namovic MT, Grayson G, Donnelly-Roberts D, Harris R, Honore P, Jarvis MF, Faltynek CR, Carroll WA (2008)
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists
Journal of Medicinal Chemistry
51 :3030
Nelson DW, Sarris K, Kalvin DM, Namovic MT, Grayson G, Donnelly-Roberts D, Harris R, Honore P, Jarvis MF, Faltynek CR, Carroll WA (2008)
Journal of Medicinal Chemistry
51 :3030