The anti-inflammatory activity of 1-methylimidazole-2-thiol (methimazo
le), the most widely used antithyroid drug, was investigated. Methimaz
ole had a marked inhibitory action on prostaglandin H synthase (IC50 =
10 mu mol/l), inhibiting the peroxidase (IC50 = 330 mu mol/l), althou
gh the cyclo-oxygenase was slightly activated. Methimazole was less po
tent than indometacin (IC50 = 1.7 mu mol/l) on prostaglandin H synthas
e, but was more potent than acetylsalicylic acid (IC50 = 160 mu mol/l)
. Methimazole has been found to trap superoxide (O-2-(radical anion))
radicals and to decrease the level of blood prostaglandin E-2.