The P2X7 receptor as a therapeutic target.
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 P2X(7) 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 P2X(7) receptor-antagonists.


METHODS
A literature review.


CONCLUSIONS
We describe the recent discoveries of novel P2X(7) receptor-selective antagonists, along with their biological activity and therapeutic potential.
Romagnoli
Romeo
R
Università di Ferrara, Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy. rmr@unife.it
Baraldi
Pier Giovanni
PG
Cruz-Lopez
Olga
O
Lopez-Cara
Carlota
C
Preti
Delia
D
Borea
Pier Andrea
PA
Gessi
Stefania
S
D000818:Animals; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000503:physiopathology; D010146:Pain / Q000188:drug therapy / Q000503:physiopathology; D058919:Purinergic P2 Receptor Antagonists; D051381:Rats; D058486:Receptors, Purinergic P2X7
C546468:P2RX7 protein, human; C546470:P2rx7 protein, rat; D058919:Purinergic P2 Receptor Antagonists; D058486:Receptors, Purinergic P2X7