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Aim:To investigate the electrophysiological effect of fluoxetine on serotonin transporter.Methods:A heterologous expression system was used to introduce human serotonin transporter(hSERT)into Xenopus oocytes.A 2-electrode voltage clamp technique was used to study the pharmacological properties of fluoxetine.Results:hSERT-expressing oocytes were perfused with 10 μmol/L serotonin (5-HT)to induce hSERT-current.The 5-HT-induced hSERT currents were dose-dependently reversed by fluoxetine.The RC50(concentration that achieved a 50% reversal)was approximately 3.12 μmol/L.Fluoxetine took more time to combine with hSERT than 5-HT did,and it was also slow to dissociate from hSERRT. This long-lasting effect of fluoxetine affected normal 5-HT transport.Fluoxetine significantly prolonged the time constant for 5-HT-induced hSERT current.These results might be used to explain the long-lasting anti-anxiety effect of fluoxetine in clinical practice,because it increases the concentration of 5-HT in the synaptic cleft by its enduring suppression of the function of 5-HT transporters.Conclusion:Fluoxetine inhibits 5-HT reuptake by competing with 5-HT and changing the normal dynamics of hSERT.