P2X Receptor Modulator

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-1β. 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).

MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).

P2X2/3 modulator-1 (Compound 46) is a P2X2/3 modulator. P2X2/3 modulator-1 can be used in the study of pain, central nervous system disorders and inflammation.