Document Detail

Inhibiting the breakdown of endogenous opioids and cannabinoids to alleviate pain.
MedLine Citation:
PMID:  22460123     Owner:  NLM     Status:  In-Data-Review    
Chronic pain remains unsatisfactorily treated, and few novel painkillers have reached the market in the past century. Increasing the levels of the main endogenous opioid peptides - enkephalins - by inhibiting their two inactivating ectopeptidases, neprilysin and aminopeptidase N, has analgesic effects in various models of inflammatory and neuropathic pain. Stemming from the same pharmacological concept, fatty acid amide hydrolase (FAAH) inhibitors have also been found to have analgesic effects in pain models by preventing the breakdown of endogenous cannabinoids. Dual enkephalinase inhibitors and FAAH inhibitors are now in early-stage clinical trials. In this Review, we compare the effects of these two potential classes of novel analgesics and describe the progress in their rational design. We also consider the challenges in their clinical development and opportunities for combination therapies.
Bernard P Roques; Marie-Claude Fournié-Zaluski; Michel Wurm
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nature reviews. Drug discovery     Volume:  11     ISSN:  1474-1784     ISO Abbreviation:  Nat Rev Drug Discov     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-03-30     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101124171     Medline TA:  Nat Rev Drug Discov     Country:  England    
Other Details:
Languages:  eng     Pagination:  292-310     Citation Subset:  IM    
1] Pharmaleads SAS, 11 Rue Watt, 75013 Paris, France. [2] Université Paris-Descartes, 4 Avenue de l'Observatoire, 75006 Paris, France.
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