GSK-1482160 (isomer)

Description

GSK-1482160 isomer is the isomer of GSK-1482160 HY-19888 . GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor P2X7R negative allosteric modulator with pIC50s of 8.5 human and 6.5 rat . GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1?. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury CCI .