Table 1.
Stimulation of release in rat brain synaptosomes
Drug | Release at DAT EC50 (nM)a |
Release at NET EC50 (nM)a |
Release at SERT EC50 (nM)a |
DAT/SERT ratiob |
---|---|---|---|---|
d-Amphetamine | 5.5 ± 0.5 | 8.2 ± 1.6 | 2602 ± 494 | 473 |
Aminorex | 9.1 ± 0.9 | 15.1 ± 3.5 | 414 ± 78 | 45 |
(±)-cis-4-MAR | 1.7 ± 0.2 | 4.8 ± 0.9 | 53.2 ± 6.8 | 31 |
(±)-cis-4,4'-DMAR | 8.6 ± 1.1 | 26.9 ± 5.9 | 18.5 ± 2.8 | 2 |
Data are expressed as mean ± SD for N = 3–4 experiments performed in triplicate.
DAT/SERT ratio calculated by (EC50 at DAT)−1/(EC50 at SERT)−1; higher value indicates greater DAT selectivity.