Recent progress in the discovery of antagonists acting at P2X(7) receptor

A review. 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 pharmacol. intervention. These findings prompted a no. of drug companies, including AstraZeneca, King and Pfizer to initiate small-mol. programs taking a no. of different approaches, which are reviewed in this review article. The extensive use of high-throughput screening approaches, utilizing diverse compd. library sources, has lead to the identification of 2 important lead series (adamantane and benzenamide derivs.) acting on P2X7.