Future Challenges
Inflammatory Diseases
There is historic expertise in inflammation and pain at the Merck Frosst Centre forTherapeutic Research, a pedigree that started with the analgesics 217® and 222® in the early 1900s (see Our Heritage).
A major focus of the laboratory has been on the inhibition of the biosynthesis of arachidonic acid metabolites or the blockade of these metabolites at their receptors. These metabolites, which include leukotrienes and prostanoids, are known to be important mediators of respiratory diseases such as asthma, as well as inflammatory disorders such as rheumatoid arthritis.
The scientists in Montréal further refined their tactics for modulating inflammation by focussing downstream in the biochemical pathway, on the prostanoid receptors. The eight currently known G-protein coupled prostanoid receptors have different selectivities for the different prostaglandins. The hope is that selective blockade of one or more of these receptors may block the negative effects of prostaglandins while retaining their positive cell-maintenance benefits.
Prostaglandin E2, known to raise temperature and intensify pain (hyperalgesia), has been a focus of interest in Montréal over the years. Blockers for receptors 1 and 3 (EP-1 and EP-3) show potential not only for pain relief but also for a number of other disorders. Exploratory projects are beginning to elucidate the physiological role of each of the eight receptors with the goal of identifying new therapeutic targets.
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217® and 222® are trademarks of Laboratoires Onil Herbert Inc.
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