Metamizole (sodium salt)

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 1-[(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]-methanesulfonic acid, monosodium salt
• Correlated keywords
  • 50567-35-6 57904-?20-?8 NSAIDs nonsteroidal anti-inflammatory antiinflammatory drugs nociceptives anti-nociceptives antinociceptives analgesics antipyretics anti-pyretics pyretics prodrugs arachidonoyl amides metabolites 4-methylaminoantipyrine MAA 4-aminoantipyrine AA cyclooxygenase1 COX-1 COX- cannabinoids CBs COXs COX1 COX2 central peripheral receptors CB1 CB2TRPV1 agranulocytosis nonspecific non-specific non specific inhibitors inhibits inhibitions pains inflammation ARPF algocalmin algocalmin algopyrin anador analgin analgine andolor conmel siprofarn gifaril lisador metamizol metapyrin methampyrone methylmelubrin metilon narone neo-melubrine neomelubrine neo melubrine noramidopyrine noraminophenazone novalgetol novalgin novaamidazophen novaminophenazone novaminsulfone restriva sodium salts sulpin sulpyrin sulpyrine dipyrone novalgin algozone algocalmin algopyrin analgin optalgin cyclooxygenase nonopioids non opioids non-opioids Dipirona Metamizol
• Product Overview:
  Metamizole is a nonopioid prodrug that is rapidly hydrolyzed to the analgesic and antipyretic metabolites 4-methylaminoantipyrine (MAA) and 4-aminoantipyrine (AA).{25749} It inhibits COX-1 and COX-2 activity (IC50 = ~150 µg/ml for both in cell-free assays), as well as reduces increases in intracellular calcium levels induced by the TRPA1 agonist AITC in isolated rat and mouse dorsal root ganglia and IMR-90 human fibroblasts (IC50s = 30-91 µM in patch-clamp assays).{46639,46640} Metamizole (6, 12, and 25 µg/ml) inhibits ADP- and epinephrine-induced platelet aggregation in human platelet-rich plasma (hPRP).{46641} It prevents fever induced by LPS, TNF-?, and IL-6, but not arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) or prostaglandin E2 (PGE2; Item No. 14010), in rats when administered at a dose of 120 mg/kg.{46642} Metamizole (250 and 500 mg/kg) increases the paw withdrawal threshold in the paw pressure test, indicating analgesic activity, in rat models of carrageenan-induced acute pain and postoperative incision pain.{46643}