TABLE 1

Affinity and potency of substituted cathinones and standard compounds at hDAT, hSERT, and hNET

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 μM, 100 μM, or 1 mM. Hill slopes for binding ranged from −0.51 to −1.69.

DrugInhibition of [125I]RTI-55 Binding Ki ± S.E.M. (n)Inhibition of [3H]Neurotransmitter Uptake IC50 ± S.E.M. (n)
hDAThSERThNEThDAT [3H]DAhSERT [3H]5-HThNET [3H]NE
μMμMμMμMμMμM
α- Pyrrolidinophenones
 α-PPP1.29 ± 0.50 (3)161.4 ± 6.7 (3)2.04 ± 0.50 (4)0.540 ± 0.076 (3)188 ± 12 (4)0.305 ± 0.057 (3)
 α-PBP0.145 ± 0.034 (7)163 ± 41 (5)0.51 ± 0.13 (5)0.078 ± 0.011 (3)67 ± 14 (5)0.143 ± 0.030 (5)
 α-PVP0.0222 ± 0.0053 (7)68 ± 18 (3)0.122 ± 0.029 (3)0.0197 ± 0.0048 (5)57 ± 14 (3)0.046 ± 0.018 (5)
 α-PHP0.0160 ± 0.0044 (8)33 ± 12 (5)0.339 ± 0.037 (9)0.0216 ± 0.0035 (6)40 ± 11 (3)0.0363 ± 0.0077 (7)
 PV-80.0148 ± 0.0041 (5)39 ± 11 (5)0.63 ± 0.14 (5)0.0145 ± 0.0016 (4)26.8 ± 7.2 (3)0.0552 ± 0.0054 (4)
 4-MePPP1.12 ± 0.14 (3)50.01 ± 0.68 (3)5.87 ± 0.45 (3)0.566 ± 0.098 (3)10.34 ± 0.68 (3)1.07 ± 0.39 (3)
 4-MeO-α-PVP0.317 ± 0.090 (5)6.07 ± 0.98 (5)1.12 ± 0.26 (5)0.1126 ± 0.0094 (3)4.18 ± 0.28 (3)0.222 ± 0.054 (3)
 3,4-MDPPP1.10 ± 0.26 (5)18.7 ± 4.9 (3)4.9 ± 1.1 (5)0.409 ± 0.068 (3)12.8 ± 1.7 (3)0.881 ± 0.074 (3)
 3,4-MDPBP0.069 ± 0.020 (3)10.14 ± 0.33 (3)0.76 ± 0.15 (5)0.057 ± 0.14 (4)3.1 ± 1.0 (3)0.146 ± 0.040 (3)
 α-PVT0.630 ± 0.054 (4)165.4 ± 5.0 (3)2.26 ± 0.31 (3)0.3428 ± 0.0049 (3)242 ± 41 (4)0.175 ± 0.038 (4)
Other substituted cathinones
 MCAT4.78 ± 0.83 (18)313 ± 46 (14)3.59 ± 0.52 (21)0.152 ± 0.015 (18)20.6 ± 3.6 (20)0.0297 ± 0.0029 (19)
 3-F-MCAT3.25 ± 0.77 (5)211 ± 48 (3)2.92 ± 0.54 (3)0.214 ± 0.056 (4)12.9 ± 3.4 (5)0.0212 ± 0.0010 (3)
 4-Cl-MCAT9.41 ± 0.65 (4)28.7 ± 5.2 (4)19.6 ± 2.6 (4)0.208 ± 0.036 (3)0.67 ± 0.13 (3)0.0755 ± 0.0072 (3)
 4-Br-MCAT7.87 ± 0.28 (3)9.24 ± 0.93 (3)17.1 ± 1.8 (3)0.471 ± 0.093 (4)0.45 ± 0.11 (8)0.070 ± 0.016 (4)
 4-MEC3.00 ± 0.52 (3)12.6 ± 2.8 (4)15.8 ± 3.9 (4)0.96 ± 0.15 (3)0.218 ± 050 (4)0.93 ± 0.23 (3)
 5-MeO-methylone144 ± 54 (4)27.9 ± 4.2 (3)76 ± 14 (3)>92 (4)1.90 ± 0.11 (4)19.0 ± 3.8 (4)
 Ethylone5.0 ± 1.6 (3)23.7 ± 2.1 (4)18.8 ± 3.0 (3)1.72 ± 0.45 (3)0.464 ± 0.075 (4)1.42 ± 0.20 (3)
 Pentedrone0.339 ± 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)
 Pentylone0.3942 ± 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)
Noncathinones
 MDAI41.3 ± 3.5 (3)119.1 ± 5.8 (3)48 ± 11 (4)3.48 ± 0.46 (3)0.59 ± 0.13 (4)0.192 ± 0.036 (3)
 4-FA33.6 ± 3.1 (4)75.8 ± 6.6 (4)18.5 ± 4.2 (3)0.091 ± 0.025 (3)3.12 ± 0.66 (4)0.0426 ± 0.0044 (3)
 METH4.58 ± 0.76 (23)213 ± 29 (20)1.82 ± 0.23 (19)0.0667 ± 0.0082 (26)7.4 ± 1.1 (27)0.0165 ± 0.0017 (23)
 MDMA32.4 ± 4.9 (15)23.9 ± 5.5 (14)26.6 ± 6.4 (16)0.410 ± 0.045 (13)0.362 ± 0.053 (14)0.108 ± 0.015 (13)
 Cocaine0.494 ± 0.037 (29)0.617 ± 0.045 (27)1.91 ± 0.23 (25)0.256 ± 0.022 (26)0.320 ± 0.034 (33)0.272 ± 0.024 (23)
 Mazindol0.0296 ± 0.0039 (20)0.085 ± 0.012 (22)0.0071 ± 0.0014 (19)0.0146 ± 0.0016 (21)0.0435 ± 0.0040 (23)0.00143 ± 0.00017 (25)
  • n, number of independent experiments conducted in duplicate.