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Dopamine transporter (DAT) inhibitors and probes act on the carrier that clears released dopamine. DAT was cloned as a cocaine-sensitive transporter, and mice lacking it show hyperlocomotion and no behavioral response to cocaine or amphetamine. The X-ray structure of the Drosophila transporter bound to an antidepressant revealed its central binding site. Listed compounds include LR1143 and SRI-32743, radafaxine hydrochloride, which inhibits dopamine and norepinephrine uptake, and DOV-102,677, which also blocks serotonin transport. IDT307 is a fluorescent transporter substrate used to measure monoamine uptake in cells.
