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In this paper we report our work on the development of a human serotonin transporter (hSERT) antagonist that can be conjugated to quantum dots. This approach has been used to target and visualize the human serotonin transporter protein (hSERT). We demonstrate that labeling is blocked by the addition of high affinity hSERT antagonists such as paroxetine. This approach may be useful for the development of fluorescent assays to study the location and temporal dynamics of biogenic amine transporters and also holds promise for the development of plate-based high throughput assays used to identify novel transporter antagonists.