Article

The P2X7 receptor as a therapeutic target.

Università di Ferrara, Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy.
Expert opinion on therapeutic targets (impact factor: 3.72). 06/2008; 12(5):647-61. DOI:10.1517/14728222.12.5.647
Source: PubMed

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.

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    Article: Purinergic receptors and pain.
    Geoffrey Burnstock
    [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
Data provided are for informational purposes only. Although carefully collected, accuracy cannot be guaranteed. The impact factor represents a rough estimation of the journal's impact factor and does not reflect the actual current impact factor. Publisher conditions are provided by RoMEO. Differing provisions from the publisher's actual policy or licence agreement may be applicable.

Keywords

appealing target
 
biological activity
 
cell types
 
current status
 
extensive use
 
hit-to-lead
 
HtL
 
HTS
 
inflammatory disorders
 
inflammatory processes
 
literature review
 
novel therapeutic approach
 
P2X7 receptor
 
selective
 
therapeutic potential