Recent progress in the discovery of antagonists acting at P2X₇ receptor

Abstract

The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, nitric oxide (NO) generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacological intervention. These findings prompted a number of drug companies, including AstraZeneca, King and Pfizer to initiate small-molecule programmes taking a number of different approaches, which are reviewed in this review article. The extensive use of high-throughput screening approaches, utilising diverse compound library sources, has lead to the identification of two important lead series (adamantane and benzenamide derivatives) acting on P2X7.

• extracellular ATP
• inflammatory process
• ionotropic receptor
• KN-62
• P2X7 (purino) receptor