RTI-336
RTI-336, -2β--3β- is a phenyltropane derivative which acts as a potent and selective dopamine reuptake inhibitor and stimulant drug. It binds to the dopamine transporter with around 20x the affinity of cocaine, however it produces relatively mild stimulant effects, with a slow onset and long duration of action. These characteristics make it a potential candidate for treatment of cocaine addiction, as a possible substitute drug analogous to how methadone is used for treating heroin abuse. RTI-336 fully substitutes for cocaine in addicted monkeys and supports self-administration, and significantly reduces rates of cocaine use, especially when combined with SSRIs, and research is ongoing to determine whether it could be a viable substitute drug in human cocaine addicts.Update
| RTI | X | R | CFT | Nisoxetine | Paroxetine | N ÷ D | S ÷ D |
| Coc | — | — | 89.1 | 3298 | 1045 | 37.01 | 11.79 |
| 177 | Cl | phenyl | 1.28 | 504 | 2420 | 393.8 | 1891 |
| 176 | Me | phenyl | 1.58 | 398 | 5110 | 251.9 | 3234 |
| 354 | Me | ethyl | 1.62 | 299 | 6400 | 184.6 | 3951 |
| 336 | Cl | p-cresyl | 4.09 | 1714 | 5741 | 419.1 | 1404 |
| 386 | Me | p-anisyl | 3.93 | 756 | 4027 | 192.4 | 1025 |
N.B. RTI-371
