Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Monoamine uptake inhibition Transporter binding affinities Transporter binding affinities
Rat brain synaptosomes Rat brain synaptosomes
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Transfected HEK293 cells
Uptake-1 Uptake-1
Uptake-1
Uptake-1
Uptake-1
Uptake-1
Uptake-2
Uptake-2
Compound [3H]DA [3H]MPP+ uptake at hDAT [3H]5-HT uptake at hSERT hDAT/hSERT ratio [3H]MPP+ uptake at hOCT-2 [3H]MPP+ uptake at hOCT-3 hDAT hSERT
Pentedrone 1.742 (1.371 – 2.112) 0.215 (0.163 – 0.267) 78.03 (69.270 – 86.790) 363 26.95 (23.996 – 29.90) > 1000 0.146 ± 0.03 11.42 ± 1.15
N-ethyl-pentedrone
0.824 (0.718 – 0.930) 0.076 (0.041 – 0.111) 78.47 (77.997 – 78.94) 1029 57.58 (46.97 – 68.19)
> 1000
0.049 ± 0.02
17.13 ± 0.9
N,N-diethyl-pentedrone
3.535 (3.175 – 3.895) 0.445 (0.325 – 0.565) > 100 > 2000
47.81 (46.745 – 48.87)
> 1000
0.398 ± 0.05
75.9 ± 36.81
α-PVP
0.139 (0.104 – 0.174) 0.032 (0.027 – 0.037) > 100 > 2000
17.49 (13.498 – 21.48)
> 1000
0.011 ± 0.004
52.2 ± 5.06
α-PpVP
1.055 (0.917 – 1.193) 0.058 (0.046 – 0.070) > 100 > 2000 12.88 (12.15 – 13.61)
> 1000
0.078 ± 0.03
> 100
Cocainea
N.A.
1.189 (0.840 – 1.68)
7.94 (6.34 – 9.94) 6.68
N.A.
N.A.
0.217 ± 0.02
N.A.
Imipraminea
N.A.
N.A.
N.A. N.A.
N.A.
N.A.
N.A.
0.010 ± 0.004