Table 1 Effect of test drugs on DAT and SERT-mediated uptake.

From: Serotonin-releasing agents with reduced off-target effects

IC50 (µM) (95% CI in brackets)

 

DAT

SERT

DAT/SERT ratio

S-MC

9.1 (6.98–11.67)

392.8 (306.3–503.6)

43.2

R-MC

10.62 (6.88–16.6)

963.7 (700.6–1332)

90.7

S-4-MMC

10.3 (6.74–16.00)

10.87 (9.18–12.93)

1.06

R-4-MMC

12.5 (6.84–23.78)

77.06 (59.63–100.2)

6.2

S-4-MC

6.65 (5.83–7.61)

12.63 (11.22–14.23)

1.9

R-4-MC

9.6 (8.1–11.41)

185.7 (166.3–207.6)

19.3

S-4-TFMMC

190.5 (120.7–310.7)

10.22 (7.9–13.34)

0.05

R-4-TFMMC

153.1 (112.7–210.9)

22.64 (19.24–26.7)

0.15

  1. Given are the IC50 values (mean and 95 CI) obtained from non-linear regression fits as shown in Fig. 1. DAT/SERT ratios were determined using the following equation: (1/DATIC50)/(1/SERTIC50). Higher values indicate higher DAT-selectivity.