TABLE 3

Potency and efficacy of substituted methcathinones and standard compounds to release preloaded [3H]neurotransmitter from HEK-hDAT, HEK-hSERT, and HEK-hNET cells

When the data could not be fit by nonlinear regression (EC50 > 10 or 100 μM), the maximum release is the average of release at the three highest concentrations tested.

DrugDrug-Induced Release of [3H]Neurotransmitter EC50 ± S.E.M. (μM) (n) % Maximum Release ± S.E.M.a
hDAT [3H]DAhSERT [3H]5-HThNET [3H]NE
α-Pyrrolidinophenones
 α-PPP>10 µM (2)>10 µM (2)>10 µM (2)
−0.51 ± 2.06%−0.58 ± 0.35%3.7 ± 4.3%
 α-PBP>100 μM (2)>100 μM (2)>100 μM (2)
−1.6 ± 2.8%1.8 ± 1.6%b−4.1 ± 4.3%
 α-PVP>100 μM (2)>100 μM (2)>100 μM (2)
4.5 ± 1.6%9.9 ± 1.5%b−1.7 ± 2.9%
 α-PHP>10 µM (2)>10 µM (2)>10 µM (2)
1.47 ± 0.59%3.2 ± 3.6%−0.5 ± 1.2%
 PV-8>10 µM (2)>10 µM (2)>10 µM (2)
−2.2 ± 0.73%−0.53 ± 1.24%17 ± 11%
 4-MePPP>100 μM (2)>100 μM (2)>100 μM (3)
−1.3 ± 1.7%−2.1 ± 1.7%b5.2 ± 2.1%
 4-MeO-α-PVP>9.5 (5)>10 µM (2)>10 µM (2)
13 ± 12%−0.5 ± 1.2%0.24 ± 0.54%
 3,4-MDPPP>10 µM (2)>10 µM (2)>10 µM (2)
1.34 ± 0.32%−1.12 ± 0.61%−0.9 ± 2.7%
 3,4-MDPBP>10 µM (2)>10 µM (2)>10 µM (2)
−0.13 ± 0.24%0.04 ± 0.54%10.2 ± 2.4%
 α-PVT>10 μM (2)>10 μM (2)>10 μM (2)
0.88 ± 0.02%0.43 ± 0.14%4.8 ± 2.7%
Other substituted cathinones
 MCAT2.31 ± 0.76 (11)107 ± 36 (7)0.64 ± 0.24 (9)
85.4 ± 6.0%65 ± 10%93.5 ± 8.2%
 3-F MCAT1.29 ± 0.42 (6)39.0 ± 4.3 (3)0.13 ± 0.05 (5)
63.3 ± 8.4%50.8 ± 1.4%b96 ± 11%
 4-Cl MCAT2.89 ± 0.99 (3)1.98 ± 0.42 (4)1.24 ± 0.44 (6)
83.5 ± 6.5%124 ± 10%84.9 ± 7.0%
 4-Br MCAT3.3 ± 1.1 (3)0.96 ± 0.13 (4)1.50 ± 0.63 (5)
90 ± 13%131 ± 13%91.8 ± 6.9%
 4-MEC>100 μM (3)1.52 ± 0.42 (3)0.71 ± 0.20 (5)
0.10 ± 2.0%99 ± 10%17.5 ± 4.2%
 5-MeO-methylone>100 μM (2)3.89 ± 0.41 (3)>100 μM (2)
2.1 ± 0.9%67.4 ± 2.5%1.6 ± 1.3%
 Ethylone>10 µM (2)1.48 ± 0.25 (4)>10 µM (2)
1.22 ± 0.62%86 ± 15%b1.3 ± 1.7%
 Pentedrone>100 μM (2)>100 μM (2)>100 μM (2)
4.2 ± 1.6%7.4 ± 2.4%b−1.1 ± 4.4%
 Pentylone>100 μM (2)>100 μM (2)>100 μM (2)
2.4 ± 1.2%−5.2 ± 2.1%b4.6 ± 1.5%
Noncathinones
 MDAI24 ± 11 (4)2.9 ± 1.2 (5)0.57 ± 0.20 (4)
25.0 ± 4.9%61 ± 12%b68 ± 18%
 4-FA1.40 ± 0.41 (5)11.1 ± 1.5 (4)0.144 ± 0.051 (5)
96 ± 15%99.5 ± 6.2%145 ± 25%
 METH0.435 ± 0.074 (13)23.3 ± 4.2 (10)0.125 ± 0.024 (8)
101.3 ± 2.993.0 ± 7.5%102.6 ± 3.0%
 MDMA7.5 ± 2.3 (10)1.10 ± 0.29 (9)0.360 ± 0.092 (7)
94 ± 10%85.1 ± 7.8%147 ± 15%
 PCA1.25 ± 0.34 (6)
105.5 ± 1.6%b
  • n, number of independent experiments.

  • a Maximum release is defined as the maximum release (maximal AUC) induced by METH (1 or 10 μM, hDAT; 0.3 or 1 μM, hNET; 0.3–1 mM, hSERT) for each experiment.

  • b Maximum release is defined as the maximum release (maximal AUC) induced by p-chloroamphetamine (PCA, 10 μM, hSERT) for each experiment.