Table 1.
Affinity and potency of substituted cathinones, benzofurans, prolintane and standard compounds at hDAT, hSERT and hNET.
| Inhibition of [125I]RTI-55 binding Ki ± sem (μΜ) (n) | Inhibition of [3H]neurotransmitter uptake IC50 ± sem (μΜ) (n) | Ratio | |||||
|---|---|---|---|---|---|---|---|
| Drug | hDAT | hSERT | hNET | hDAT [3H]DA | hSERT [3H]5-HT | hNET [3H]NE | DAT/SERT |
| α- pyrrolidinophenones | |||||||
| α-PVPa | 0.0222 ± 0.0053 (7) | 68 ± 18 | 0.122 ± 0.029 (3) | 0.0197 ± 0.0048 (5) | 57 ± 14 (3) | 0.046 ± 0.018 (5) | 2900 |
| 4-Cl-α-PPP | 1.30 ± 0.45 (5) | 12.7 ± 3.2 (3) | 3.58± 0.92 (5) | 0.73 ± 0.13 (4) | 6.4 ± 1.5 (3) | 1.42 ± 0.38 (5) | 8.8 |
| 4-F-α-PVP | 0.376 ± 0.070 (5) | 14.7 ± 1.6 (6) | 1.10 ± 0.10 (4) | 0.119 ± 0.025 (3) | 42.5 ± 6.0 (4) | 0.118 ± 0.017 (3) | 360 |
| 4-Cl-α-PVP | 0.061 ± 0.015 (4) | 2.02 ± 0.19 (4) | 0.281 ± 0.016 (4) | 0.0248 ± 0.0014 (3) | 2.07 ± 0.33 (3) | 0.0291 ± 0.0067 (3) | 83 |
| 4-F-α-PHP | 0.122 ± 0.027 (6) | 8.01 ± 0.84 (5) | 1.73 ± 0.25 (4) | 0.0382 ± 0.0044 (4) | 9.11 ± 0.54 (4) | 0.218 ± 0.029 (3) | 240 |
| 4-Me-α-PHP | 0.0230 ± 0.0062 (4) | 4.78 ± 0.26 (3) | 0.75 ± 0.16 (4) | 0.0132 ± 0.0036 (4) | 1.58 ± 0.40 (5) | 0.042 ± 0.011 (4) | 120 |
| 3,4-MDPHP | 0.0192 ± 0.0051 (3) | 2.43 ± 0.51 (3) | 0.935 ± 0.093 (3) | 0.0084 ± 0.0022 (3) | 1.34 ± 0.41 (3) | 0.047 ± 0.010 (3) | 160 |
| PV9 | 0.0180 ± 0.0037 (5) | 2.86 ± 0.43 (3) | 0.468 ± 0.033 (3) | 0.0502 ± 0.0066 (3) | >7.4 μM | 0.0304 ± 0.0.0059 (3) | >150 |
| TH-PVP | 3.09 ± 0.30 (4) | 0.131 ± 0.028 (3) | 6.95 ± 0.34 (3) | 2.40 ± 0.11 (3) | 0.208 ± 047 (5) | 2.129 ± 0.081 (3) | 0.087 |
| Other cathinones | |||||||
| Pentedronea | 0.339 ± 0.098 (7) | 16.4 ± 4.6 (3) | 1.95 ± 0.56 (5) | 0.1762 ± 0.0089 (3) | 9.0 ± 2.3 (3) | 0.239 ± 0.067 (3) | 51 |
| 4-MPD | 1.45 ± 0.31 (3) | 6.2 ± 1.4 (6) | 3.39 ± 0.48 (3) | 0.188 ± 0.03 (3) | 0.532 ± 0.016 (3) | 0.307 ± 0.061 (3) | 2.8 |
| 4-CPD | 1.62 ± 0.40 (4) | 3.85 ± 0.55 (3) | 4.54 ± 0.89 (3) | 0.486 ± 0.067 (3) | 0.61 ± 0.15 (3) | 0.47 ± 0.14 (4) | 1.3 |
| α-EPP | 0.182 ± 0.022 (4) | 8.4 ± 2.1 (5) | 0.70 ± 0.18 (3) | 0.165 ± 0.043(3) | 10.5 ± 2.0 (3) | 0.101 ± 0.024 (3) | 64 |
| N-propyl pentedrone | 0.389 ± 0.067 (3) | >30 μM (3) | 3.76 ± 0.82 (3) | 0.127 ± 0.023 (3) | 42.0 ± 4.9 (4) | 0.306 ± 0.079 (3) | 330 |
| 4-MEAP | 0.123 ± 0.026 (3) | 0.765 ± 0.073 (3) | 0.576 ± 0.085 (3) | 0.179 ± 0.034 (3) | 1.14 ± 0.12 (3) | 0.083 ± 0.018 (5) | 6.4 |
| N-Et-Hexedrone | 0.171 ± 0.038 (3) | 11.4 ± 1.8 (3) | 1.259 ± 0.043 (3) | 0.0467 ± 0.0040 (3) | 4.88 ± 0.47 (3) | 0.0978 ± 0.0083 (3) | 100 |
| Pentylonea | 0.3942 ± 0.0040 (3) | 3.38 ± 0.52 (4) | 8.19 ± 0.57 (3) | 0.167 ± 0.037 (3) | 0.81 ± 0.14 (4) | 0.65 ± 0.16 (3) | 4.9 |
| N-Et pentylone | 0.102 ± 0.015 (4) | 0.893 ± 0.080 (3) | 2.38 ± 0.62 (3) | 0.0549 ± 0.0073 (3) | 0.46 ± 0.12 (4) | 0.114 ± 0.029 (6) | 8.4 |
| bk-DMBDP | 0.354 ± 0.073 (3) | 2.27 ± 0.30 (3) | 2.00 ± 0.14 (3) | 0.233 ± 0.066 (3) | 2.57 ± 0.55 (5) | 0.212 ± 0.068 (4) | 11 |
| Dibutylone | 0.581 ± 0.076 (4) | >10 μM (2) | 8.4 ± 2.1 (3) | 0.302 ± 0.013 (3) | >9.7 μM (3) | 0.923 ± 0.044 (3) | >32 |
| Dimethylone | 4.21 ± 0.27 (3) | >10 μM (3) | >10 μM (2) | 2.22 ± 0.36 (3) | >9.2 μM (3) | 4.20 ± 0.88 (4) | >4.1 |
| PRONE | 6.8 ± 1.9 (3) | 13.3 ± 1.0 (3) | 22.5 ± 8.5 (3) | 2.38 ± 0.46 (3) | 2.25 ± 0.35 (3) | 6.04 ± 0.89 (3) | 0.95 |
| MCAT | 7.52 ± 0.99 (17) | 312 a±34 (18) | 5.96 ± 0.61 (17) | 0.225 ± 0.038 (23) | 29.4 ± 6.7 (22) | 0.0452 ± 0.0042 (19) | 130 |
| 3-MMC | 6.33 ± 0.72 (3) | 7.9 ± 1.8 (4) | 2.85 ± 0.72 (4) | 0.433 ± 0.089 (3) | 4.5 ± 1.3 (5) | 0.084 ± 0.023 (5) | 10 |
| 4-CEC | 4.17 ± 0.53 (3) | 7.9 ± 1.2 (3) | 16.3 ± 5.7 (5) | 0.931 ± 0.080 (3) | 0.36 ± 0.10 (5) | 1.72 ± 0.24 (3) | 0.39 |
| Mexedrone | 8.39 ± 0.54 (3) | 22.2 ± 6.2 (3) | >27.6 μM (2) | 2.75 ± 0.22 (3) | 5.4 ± 1.2 (3) | 3.19 ± 0.98 (5) | 2.0 |
| Benzofurans | |||||||
| 2-MAPB | 1.63 ± 0.44 (3) | 2.97 ± 0.18 (3) | 1.99 ± 0.22 (3) | 0.233 ± 0.061 (5) | 0.693 ± 0.068 (3) | 0.0393 ± 0.0052 (3) | 3.0 |
| 5-MAPB | 2.66 ± 0.61 (3) | 1.39 ± 0.33 (3) | 3.15 ± 0.27 (3) | 0.099 ± 0.010 (3) | 0.137 ± 0.024 (3) | 0.073 ± 0.018 (3) | 1.4 |
| 6-MAPB | 0.5993 ± 0.0099 (3) | 3.85 ± 0.66 (3) | 1.48 ± 0.27 (3) | 0.052 ± 0.017 (4) | 0.496 ± 0.074 (3) | 0.0331 ± 0.0020 (3) | 9.5 |
| 6-APB | 1.04 ± 0.16 (4) | 2.75 ± 0.62 (3) | 2.45 ± 0.20 (4) | 0.121 ± 0.022 (4) | 0.290 ± 0.062 (4) | 0.0198 ± 0.0044 (4) | 2.4 |
| 6-EAPB | 0.089 ± 0.022 (3) | 1.31 ± 0.25 (3) | 0.772 ± 0.044 (3) | 0.051 ± 0.012 (4) | 0.0719 ± 0.0094 (5) | 0.042 ± 0.014 (4) | 1.4 |
| 5-MAPDB | >30 μM (3) | 8.8 ± 1.7 (4) | >30 μM (3) | 2.79 ± 0.80 (3) | 0.113 ± 0.030 (4) | 0.56 ± 0.18 (3) | 0.041 |
| Other noncathinones | |||||||
| Prolintane | 0.219 ± 0.019 (3) | 2.52 ± 0.33 (3) | 0.56 ± 0.19 (3) | 0.100 ± 0.021 (3) | 1.11 ± 0.35 (6) | 0.0460 ± 0.0068 (3) | 11 |
| METH | 4.41 ± 0.43 (20) | 150 ± 17 (20) | 2.51 ± 0.24 (16) | 0.097 ± 0.013 (21) | 9.3 ± 1.1 (18) | 0.0258 ± 0.0030 (19) | 96 |
| MDMA | 31.0 ± 4.9 (6) | 17.5 ± 3.3 (6) | 15.8 ± 4.1 (7) | 0.479 ± 0.070 (4) | 0.118 ± 0.019 (4) | 0.63 ± 0.14 (3) | 0.25 |
| Cocaine | 0.495 ± 0.049 (22) | 0.495 ± 0.034 (20) | 1.95 ± 0.15 (18) | 0.425 ± 0.036 (23) | 0.364 ± 0.040 (24) | 0.382 ± 0.037 (23) | 0.86 |
(n) Number of independent experiments conducted in duplicate.
Data are normalized to specific binding or specific uptake in the absence of drugs. Drugs were tested in binding and uptake assays at concentrations ranging from 1 nM to 10 μΜ, 100 μΜ or 1 mM.
a
Data from (Eshleman et al. 2017), with permission.