Table 1.
Range of previously reported IC50 values for neurotransmitter uptake inhibition.
| Cocaine | MDPV | d-Amphetamine | MDMA | Fenfluramine | Mephedrone | |
|---|---|---|---|---|---|---|
| IC50 (µM) | ||||||
| SERT | ||||||
| HEK 293 | 0.3–2.41 | 1.4–122 | > 10–1103 | 0.1–1214 | 1.15 | 0.5–266 |
| Synaptosomes | 0.3–1.07 | 3.38 | 3.4–8.09 | 0.1–4.110 | 0.5–511 | 0.3–0.612 |
| DAT | ||||||
| HEK 293 | 0.3–1.313 | 0.01–0.0514 | 1.3–7.515 | 0.2–4316 | 0.1–98.817 | |
| Synaptosomes | 0.2–1.018 | 0.004–0.00519 | 0.093–0.09420 | 1.0–3.921 | 13.8–21.522 | 0.5–1.123 |
| NET | ||||||
| HEK 293 | 0.2–1.924 | 0.02–0.0425 | 0.07–1.526 | 0.02–12.427 | 0.05–6.828 | |
| Synaptosomes | 0.3–0.429 | 0.02–0.0330 | 0.0731 | 0.532 | 8.033 | 0.2–0.534 |
Each concentration range was derived from various studies (indicated by superscripts). Baumann et al. (2013): 7,8,9,10,12,18,19,20,21,23,29,30,31,32,34, Hadlock et al. (2011): 7,18,10,21,12,23, Reith et al. (2015): 19, Bogen et al. (2003): 10,21, Kolanos et al. (2015): 18,19,29,30, Rickli et al. (2015): 2,3,4,14,15,16,25,26,27, Cameron et al. (2013): 13,14,17, Lopez-Arnau et al. (2012): 12,23,34, Rosenauer et al. (2013): 3,4,6,15,16,17,26,27,28, Cozzi et al. (1998): 11,22,33, Luethi et al. (2018a): 1,13,24, Rothman et al. (2015): 7,18,29, Escubedo et al. (2011): 10,21, Luethi et al. (2018b): 6,17,28, Sandtner et al. (2016): 4, Eshleman et al. (2013): 1,2,4,6,13,14,16,17,24,25,27,28, Luethi et al. (2019a): 2,4,14,16,25,27, Scholze et al. (2000): 5, Eshleman et al. (2017): 1,4,13,16,24,27, Mayer et al. (2016): 6,17,28, Simmler et al. (2013): 1,2,3,4,6,13,14,15,16,17,24,25,26,27,28, Fleckenstein et al. (1999): 7,9,11,18,20,22, McLaughlin et al. (2017): 12,23,34, Verrico et al. (2007): 4,16,27, Gobbi et al. (2002): 10, Pifl et al. (2015): 4,6,16,17,27,28, Zwartsen et al. (2017): 1,3,4,13,15,16,24,26,27, MDPV, 3,4-methylenedioxypyrovalerone; MDMA, 3,4-methylenedioxymethamphetamine; HEK, human embryonic kidney.