Antinociceptive Activity of Metamizol Metabolites in a Rat Model of Arthritic Pain

作者：Javier Lopez Munoz Francisco; Soria Arteche Olivia; Medina Lopez Jose Raul; Hurtado y de la Pena Marcela; Lozada Garcia Ma Concepcion; Alfonso Moreno Rocha Luis; Miriam Dominguez Ramirez Adriana

来源：Drug Development Research, 2013, 74(5): 332-338.

DOI：10.1002/ddr.21083

• metamizol
• metabolites
• synthesis
• antinociception
• PIFIR model

The aim of the present study was to evaluate the antinociceptive activity of the main metamizol (MET) metabolites, 4-methylaminoantipyrine (MAA), 4-aminoantipyrine (AA), 4-formylaminoantipyrine (FAA), and 4-acetylaminoantipyrine (AAA) using the pain-induced functional impairment in rat model (PIFIR model). The antinociceptive efficacies of MAA and AA were 288.3%h and 281.1%h, respectively, close to the efficacy of MET (333.80%h). The effective dose to attain 50% of the maximum response (ED50) values for MET, MAA and AA were 126.1, 124.9, and 110.7mg/kg, respectively. FAA and AAA were essentially inactive in this experimental model. Part of the antinociceptive effect showed by MET in this study might be attributed to the effect of the metabolites MAA and AA on cyclooxygenases COX-1 and COX-2 activity.

• 出版日期2013-8