TABLE 1

Effects of amphetamine and PEA analogs on the uptake of [3H]neurotransmitters and on the release of [3H]MPP+ at DAT or NET in rat brain synaptosomes

Data are means ± S.D. for N = 3 experiments performed in triplicate. %Emax is defined as the percentage of maximal releasing response induced by 10 µM tyramine. DAT/NET ratio = (DAT IC50−1)/(NET IC50−1); higher value indicates greater DAT selectivity.

DrugUptake Inhibition at DAT [IC50 (nM)]Uptake Inhibition at NET [IC50 (nM)]DAT/NET Ratio
Amphetamine122 ± 1269 ± 90.56
AEPEA3366 ± 333573 ± 780.16
MEPEA2248 ± 245503 ± 950.22
DEPEA510 ± 38427 ± 600.84
Release at DAT EC50 (nM) (%Emax)Release at NET EC50 (nM) (%Emax)
Amphetamine5 ± 1 (102)8 ± 1 (96)1.6
AEPEA273 ± 36 (101)80 ± 17 (100)0.29
MEPEA179 ± 25 (101)58 ± 12 (96)0.32
DEPEA604 ± 159 (43)209 ± 35 (82)0.35