A review. The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, NO generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacol. intervention. The characterization of native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtype-selective agonists and antagonists. BzATP is currently the most potent agonist known at the endogenous and recombinant P2X7 receptor A tyrosine deriv. named KN-62 exhibits selective P2X7 receptor-blocking properties. In this review article we have reported novel series of KN-62-related compds. of the general structure R1-Tyr(OR2)-piperazinyl-R3, in which three positions (R1, R2 and R3) were systematically varied. Two recent articles published by AstraZeneca have reported that novel series of cyclic imides and adamantane amides are potent P2X7 receptor antagonists.
Agonists and antagonists acting at P2X(7) receptor
BARALDI, Pier Giovanni;DI VIRGILIO, Francesco;ROMAGNOLI, Romeo
2004
Abstract
A review. The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, NO generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacol. intervention. The characterization of native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtype-selective agonists and antagonists. BzATP is currently the most potent agonist known at the endogenous and recombinant P2X7 receptor A tyrosine deriv. named KN-62 exhibits selective P2X7 receptor-blocking properties. In this review article we have reported novel series of KN-62-related compds. of the general structure R1-Tyr(OR2)-piperazinyl-R3, in which three positions (R1, R2 and R3) were systematically varied. Two recent articles published by AstraZeneca have reported that novel series of cyclic imides and adamantane amides are potent P2X7 receptor antagonists.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
