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In order to study the pharmacological action site of auranofin during the functional suppression of leukocytes, especially neutrophils, we investigated the influence of auranofin on the calcium-45 (45Ca2+) uptake into peripheral blood neutrophils and peritoneal resident macrophages isolated from normal and adjuvant-induced arthritis (AA) rats. Calcium-45 uptake into neutrophils and macrophages obtained from normal and AA rats was increased by stimulation with opsonized-zymosan, while auranofin inhibited the increase in the 45Ca2+ uptake into neutrophils, but not into macrophages. There was a tendency that auranofin more strongly inhibited the increase in the 45Ca2+ uptake into neutrophils obtained from AA rats than normal rats, but no statistically significant difference between them was observed in the inhibitory potency of auranofin. From these results, it is suggested that auranofin would show anti-rheumatic and anti-inflammatory effects by the inhibition of Ca2+ uptake into neutrophils which infiltrate into local lesions during the early and active phases of rheumatoid arthritis.