Table 2.
Affinity and potency of substituted methcathinones and standard compounds at hDAT, hSERT and hNET.
| Inhibition of [125I]RTI-55 binding Ki ± sem (µM)(n) |
Inhibition of [3H]neurotransmitter uptake IC50 ± sem (µM)(n) |
|||||
|---|---|---|---|---|---|---|
| Drug | hDAT | hSERT | hNET | hDAT [3H]DA | hSERT [3H]5-HT | hNET [3H]NE |
| Butylone | 1.73 ± 0.27(7) | 10.5 ± 1.9(5) | 7.98 ± 0.55 (3) | 0.211 ± 0.054(6) | 1.97 ± 0.43(5) | 1.06 ± 0.24 (4) |
| 4-FMC | 10.4 ± 3.3(6) | >100 µM(6) | 35 ± 10(6) | 0.273 ± 0.074 (4) | >10 µM(3) | 0.127 ± 0.020(4) |
| MDPV | 0.0194 ± 0.0032 (3) | 1.25 ± 0.21 (3) | 0.107 ± 0.034 (3) | 0.0126 ± 0.0024(3) | 1.38 ± 27(3) | 0.0188 ± 0.0021 (3) |
| Mephedrone | 4.80 ± 0.75 (3) | 21.0 ± 4.8(4) | 11.8 ± 4.0(4) | 0.098 ± 0.027 (4) | 0.51 ± 0.15(5) | 0.0536 ± 0.0087 (3) |
| Methylone | 5.02 ± 0.29 (3) | 95.5 ± 4.3 (3) | 16.5 ± 4.9(6) | 0.343 ± 0.024 (4) | 1.92 ± 0.35(5) | 0.234 ± 0.055 (8) |
| Naphyrone | 0.01077 ± 0.00076 (3) | 0.0149 ± 0.0042 (3) | 0.059 ± 0.015(3) | 0.0126 ± 0.0031 (5) | 0.0593 ± 0.0097 (4) | 0.035 ± 0.014(11) |
| METH | 3.96 ± 0.92 (3) | 240.5 ± 8.9 (3) | 1.39 ± 0.12(6) | 0.026 ± 0.010(4) | 4.1 ± 1.3(7) | 0.0260 ± 0.0077 (6) |
| MDMA | 22.0 ± 5.1 (3) | 14.7 ± 2.9(4) | 30.9 ± 5.6 (3) | 0.201 ± 0.047(5) | 0.109 ± 0.017 (5) | 0.0242 ± 0.0050 (4) |
| Methcathinone | 3.3 ± 1.1 (3) | >100 µM(3) | 4.48 ± 0.49 (6) | 0.144 ± 0.032 (4) | 13.5 ± 2.9(6) | 0.0311 ± 0.0051(3) |
| Cocaine | 0.558 ± 0.082 (10) | 0.234 ± 0.036(5) | 1.38 ± 0.29 (7) | 0.370 ± 0.072 (9) | 0.257 ± 0.048 (7) | 0.217 ± 0.025(8) |
| Mazindol | 0.041 ± 0.019(9) | 0.026 ± 0.012(4) | 0.0054 ± 0.0016(7) | 0.0300 ± 0.0081 (7) | 0.0307 ± 0.0055 (3) | 0.00185 ± 0.00049 (9) |
(n) Number of independent experiments conducted in duplicate (binding) or triplicate (uptake).
Data are normalized to specific binding or specific uptake in the absence of drugs. Drugs were tested in binding assays at concentrations ranging from 1 nM to either 10 µM or 100 µM. Hill slopes for binding ranged from −0.58 to −1.23.