Background: The P2X7 receptor is present in a variety of cell types involved in pain, inflammatory processes and neurodegenerative conditions, thus it may be an appealing target for pharmacological intervention. The extensive use of high-throughput screening (HTS) followed by a hit-to-lead (HtL) program, has prompted a number of firms to identify highly selective and metabolically stable small-molecules possessing activity for both the rat and human P2X7 receptor, which provide a novel therapeutic approach to the treatment of pain as well as neurodegenerative and inflammatory disorders. Objective: To describe the current status of and potential for development of P2X7 receptor-antagonists. Methods: A literature review. Results/conclusions: We describe the recent discoveries of novel P2X7 receptor-selective antagonists, along with their biological activity and therapeutic potential.
The P2X7 receptor as a therapeutic target.
ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;BOREA, Pier Andrea;GESSI, Stefania
2008
Abstract
Background: The P2X7 receptor is present in a variety of cell types involved in pain, inflammatory processes and neurodegenerative conditions, thus it may be an appealing target for pharmacological intervention. The extensive use of high-throughput screening (HTS) followed by a hit-to-lead (HtL) program, has prompted a number of firms to identify highly selective and metabolically stable small-molecules possessing activity for both the rat and human P2X7 receptor, which provide a novel therapeutic approach to the treatment of pain as well as neurodegenerative and inflammatory disorders. Objective: To describe the current status of and potential for development of P2X7 receptor-antagonists. Methods: A literature review. Results/conclusions: We describe the recent discoveries of novel P2X7 receptor-selective antagonists, along with their biological activity and therapeutic potential.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
