TABLE 1.
In vitro potency of PAL analogs as releasers of monoamine neurotransmitters
These data are adapted from Wee et al. (2005) and Rothman et al. (2005). DA/NE ratio was calculated by EC50−1 for DA release/EC50−1 for NE release; DA/5-HT ratio was calculated by EC50−1 DA release/EC50−1 for 5-HT release. Higher ratios indicate higher DA selectivity.
Drug | EC50 (nM ± S.D.) |
DA/NE Ratio | DA/5-HT Ratio | ||
---|---|---|---|---|---|
[3H]DA | [3H]NE | [3H]5-HT | |||
(+)-Amphetamine | 8.0 ± 0.43 | 7.2 ± 0.44 | 1756 ± 94 | 0.91 | 219 |
PAL-353 | 24.2 ± 1.1 | 16.1 ± 1.7 | 1937 ± 202 | 0.67 | 80 |
PAL-303 | 51.5 ± 1.7 | 28.0 ± 1.8 | 939 ± 76 | 0.56 | 18 |
PAL-314 | 33.3 ± 1.3 | 18.3 ± 1.4 | 218 ± 22 | 0.55 | 6.5 |
PAL-313 | 44.1 ± 2.6 | 22.2 ± 1.3 | 53.4 ± 4.1 | 0.50 | 1.2 |