TABLE 1

Summary of BAT release assays

DrugStructureDATSERTNET
EC50EMAXEC50EMAXEC50EMAX
nM ± S.D.% ± S.D.nM ± S.D.% ± S.D.nM ± S.D.% ± S.D.
D-AmphetamineEmbedded Image6.4 ± 1103 ± 51960 ± 140a104 ± 27.4 ± 2.42101 ± 10
PAL-192 (±)-MDEEmbedded Image622 ± 12161 ± 2*47 ± 1094 ± 42608 ± 53785 ± 4
PAL-193 (+)-MDEEmbedded Image507 ± 8365 ± 2*52 ± 997 ± 4651 ± 11793 ± 3
PAL-194b (−)-MDEEmbedded ImageUptake inhibitor465 ± 6989 ± 3*Uptake inhibitor
PAL-287cEmbedded Image15.7 ± 1.0102 ± 13.9 ± 0.4107 ± 39.8 ± 1.596 ± 3
PAL-1046Embedded Image10 ± 1101 ± 313 ± 2103 ± 534 ± 398 ± 2
PAL-1045Embedded Image46 ± 1178 ± 5*12 ± 266 ± 2*137 ± 3094 ± 4
PAL-218Embedded Image1207 ± 11866 ± 1*26 ± 785 ± 4*56 ± 1262 ± 3*
PAL-738Embedded Image58 ± 1078 ± 2*23 ± 296 ± 265 ± 1289 ± 3
PAL-153Embedded Image>10,000561 ± 17254 ± 3*>10,000
PAL-175Embedded Image>10,00043 ± 1657 ± 4*>10,000
PAL-179Embedded Image>10,00033 ± 966 ± 3*>10,000
PAL-874Embedded Image688 ± 11092 3>10,000305 ± 3675 ± 2*
PAL-1062Embedded Image75 ± 3751 ± 4*
PAL-1063Embedded Image21 ± 393 ± 3
  • a Data taken from Rothman et al. (2001).

  • b PAL-194 was an uptake inhibitor at DAT (IC50 = 4256 ± 191 nM) and NET (IC50 = 3973 ± 455 nM).

  • c Data taken from Rothman et al. (2005). These results differ slightly from the published values because the original data set was fit to a two-parameter logistic equation rather than the dose-response curve equation.

  • * P < 0.05 compared with 100 ± 5% (DAT, SERT) and 100 ± 10% (NET) using a one-sample Student's t test. In this test, the test is between the observed EMAX (± S.D.) and 100% ± (average S.D. observed in these assays).