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Endomorphins: Improved analgesia and anti-inflammatory molecules LeadDiscovery has, in a recent DiscoveryDossier, analyzed the therapeutic potential of the casomorphins. These peptides are liberated from beta-casein and alpha-s1-casein and bind to opiate receptors. Bristol University researchers have now described the anti-inflammatory activity of related opioids, endomorphin (EM)-1 and –2. These recently discovered peptides have been proposed as endogenous ligands for mu opioid receptors displaying high selectivity for this subtype. A model of inflammatory pain has been shown to increase both mu opioid receptor and EM-1 expression (on peripheral/central nerve terminals and macrophage/monocytes respectively). Furthermore, EM-1 is able to increase pain threshold in a model of arthritis and also to reduce cytokine release by macrophages. Now for the first time Bristol University researchers have identified these peptides in human lymphocytes. This group has also demonstrated EM-1 over-expression by synovial tissue sampled from rats with experimental rheumatoid arthritis further suggesting a therapeutic role for EM-1 mimics in the treatment of inflammatory conditions associated with pain. This peptide does not however appear to act via the same mu opioid receptor subtype as morphine and may therefore offer analgesia without the limitations of morphine. This would be of significant appeal to conditions such as rheumatoid arthritis. This condition affects about 1% of all populations, women two to three times more often than men. This translates to a total of 5 million sufferers in the major pharmaceutical markets. The market for agents used to treat rheumatoid arthritis totaled $1.6 billion in 2000, and is expected to grow at a rate of over 15% by 2006. At present, treatments of this disease are based on symptomatic therapies such as NSAIDs (including the new COX-2 inhibitors), gold-containing compounds and corticosteroids. The current trend is to move towards disease-modifying anti-rheumatic drugs (DMARDs) that generally act to modulate the immune response and therefore the ability of EM-1 mimics to reduce pain and inflammation may be of particular benefit. Entry date September, 2002 Adapted from Jessop et al, Ann N Y Acad Sci 2002 Jun;966:456-63
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