Cocaine displaces [3H]WIN 35,428 binding to dopamine uptake sites in vivo more rapidly than mazindol or GBR 12909.

Previous studies have shown that [3H] WIN 35,428 binds preferentially to striatal cocaine receptors at the dopamine transporter after in vivo injection. In vivo binding competition studies were carried out to assess the relative rates of entry and occupancy of cocaine receptors by (-)-cocaine, mazindol and GBR 12909. After i.v. injection, (-)-cocaine occupied receptors relatively more rapidly than GBR 12,909 while mazindol was the slowest.