A nonopioid prodrug
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Metamizole (sodium salt) is a nonopioid prodrug that is rapidly hydrolyzed to the metabolites 4-methylaminoantipyrine (MAA) and 4-aminoantipyrine (AA), which have analgesic and antipyretic effects. MAA has been shown to inhibit COX activity 8-9-fold more potently than AA (COX-1: IC50s = 2.6 and 20.8 µM, respectively, and COX-2: IC50s = 4.7 and 41.8 µM, respectively). These metabolites can be further acylated with arachidonic acid to form compounds that can bind to central and peripheral cannabinoid (CB1 and CB2) receptors and TRPV1 receptors at low micromolar concentrations.
LX1606 Hippurate (Telotristat etiprate)
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