The P2X7 receptor as a therapeutic target.
ABSTRACT 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.
To describe the current status of and potential for development of P2X(7) receptor-antagonists.
A literature review.
We describe the recent discoveries of novel P2X(7) receptor-selective antagonists, along with their biological activity and therapeutic potential.
Article: Purinergic receptors and pain.[show abstract] [hide abstract]
ABSTRACT: There is a brief summary of the early background literature about purinergic signalling and its involvement in pain, of ATP storage, release and ectoenzymatic breakdown and of the current classification of receptor subtypes for purines and pyrimidines. The review then focuses on purinergic mechanosensory transduction involved in visceral, cutaneous and musculoskeletal nociception and on the roles played by P2X-(3), P2Y(2/3), P2X(4), P2X(7) and P2Y(12) receptors in neuropathic and inflammatory pain. Current developments of compounds for the therapeutic treatment of both visceral and neuropathic pain are discussed.Current pharmaceutical design 02/2009; 15(15):1717-35. · 4.41 Impact Factor