TABLE 2

hDAT uptake selectivity and ratio of binding affinity to uptake potency of substituted cathinones and standard compounds at hDAT, hSERT, and hNET

DrughDAT Uptake SelectivityaRatio of Ki for Inhibition of [125I]RTI-55 Binding/IC50 for Inhibition of [3H]Neurotransmitter Uptake
hDAThSERThNET
α-Pyrrolidinophenones
 α-PPP3482.40.96.7
 α-PBP8591.92.43.6
 α-PVP28931.11.22.7
 α-PHP18520.70.89.3
 PV-818481.01.511.4
 4-MePPP18.32.04.85.5
 4-MeO-α-PVP37.12.81.55.0
 3,4-MDPPP31.32.71.55.6
 3,4 MDPBP54.41.23.35.2
 α-PVT7061.80.712.9
 MDPV110b1.5b0.91b5.7b
 Naphyrone4.7b0.85b0.25b1.7b
Other substituted cathinones
 MCAT13631.415.2120.9
 3-F MCAT60.315.216.4137.7
 4-Cl MCAT3.2245.242.8259.6
 4-Br MCAT0.9616.720.5244.3
 4-MEC0.233.157.817.0
 5-MeO-methylone<0.02<1.614.74.0
 Ethylone0.272.951.113.2
 Pentedrone51.11.91.88.2
 Pentylone4.92.44.212.6
 4-F MCAT>36b38bND276b
 Butylone9.3b8.2b5.3b7.5b
 Mephedrone5.2b49b41b220b
 Methylone5.6b15b50b71b
Noncathinones
 MDAI0.1711.9201.9250
 4-FA34.3369.224.3434.3
 METH11168.728.8110.3
 MDMA0.8879.066.0246.3
 Cocaine1.251.91.97.0
 Mazindol3.02.02.05.0
  • 4-F MCAT, 4-fluoromethcathinone; Mephedrone, 4-methyl-N-methylcathinone; ND, ratio could not be determined.

  • a hDAT uptake selectivity is calculated as 1/hDAT IC50:1/hSERT IC50.

  • b Data from Eshleman et al. (2013).