A prostaglandin antagonist is a hormone antagonist acting upon one or more prostaglandins, a subclass of eicosanoid compounds which function as signaling molecules in numerous types of animal tissues. NSAIDs are perhaps the best-known prostaglandin antagonists; they suppress the signaling function of prostaglandins, which are important mediators of pain, fever, and inflammation responses, by inhibiting the cyclooxygenase enzymes and thereby reducing prostaglandin synthesis. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein. Relatively new NSAIDs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of the COX-2 isoform of cyclooxygenase. The development of these drugs allowed the circumvention of the neg
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| - A prostaglandin antagonist is a hormone antagonist acting upon one or more prostaglandins, a subclass of eicosanoid compounds which function as signaling molecules in numerous types of animal tissues. NSAIDs are perhaps the best-known prostaglandin antagonists; they suppress the signaling function of prostaglandins, which are important mediators of pain, fever, and inflammation responses, by inhibiting the cyclooxygenase enzymes and thereby reducing prostaglandin synthesis. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein. Relatively new NSAIDs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of the COX-2 isoform of cyclooxygenase. The development of these drugs allowed the circumvention of the neg (en)
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| - A prostaglandin antagonist is a hormone antagonist acting upon one or more prostaglandins, a subclass of eicosanoid compounds which function as signaling molecules in numerous types of animal tissues. NSAIDs are perhaps the best-known prostaglandin antagonists; they suppress the signaling function of prostaglandins, which are important mediators of pain, fever, and inflammation responses, by inhibiting the cyclooxygenase enzymes and thereby reducing prostaglandin synthesis. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein. Relatively new NSAIDs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of the COX-2 isoform of cyclooxygenase. The development of these drugs allowed the circumvention of the negative gastrointestinal side effects of NSAIDs while still effectively reducing inflammation. Prostaglandin antagonists may also help with allergies, primarily seasonal allergies or nasal allergies. The prostaglandin D2 (PGD2) receptor is activated when it comes into contact with PGD2 which is released in the presence of allergens. A research study has been conducted to find an antagonist to the PGD2 receptor, DP1, to possibly treat congestion. ONO-4053 is an antagonist that was used on dogs to help with allergic rhinitis caused by PGD2. The study showed that ONO-4053 given either orally or through IV greatly helped increase nasal volume and possibly relieve rhinorrhea by blocking the PGD2 receptor before it can be activated by PGD2. Similarly, to how PGD2 antagonists can minimizing symptoms caused by allergies, prostaglandin E2 (PGE2) antagonists can also decrease inflammation, swelling, and pain caused by osteoarthritis. A study was made to see the effect of grapiprant, a prostaglandin EP4 receptor antagonist, which uses allosteric inhibition to prevent PGE2 to bind to its receptor as opposed to generally blocking viable receptors such as prostaglandin endoperoxide synthase or cyclooxygenase. Studies have shown that grapiprant can be used to treat pain and inflammation similar to NSAIDs that are prescribed to dogs with osteoarthritis. NSAIDs interfere with the cyclooxygenase and levels of various chemical mediators which may lead to a disruption in the body’s homeostasis. Grapiprant is able to selectively bind to only the EP4 receptor and minimize any adverse reactions that may occur. (en)
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