TABLE 1

Effects of synthetic cathinones analogs on inhibition of [3H]neurotransmitter uptake and release of [3H]MPP+ via DAT and NET or [3H]5-HT via SERT in rat brain synaptosomes

Data are mean ± S.D. for n = 3 experiments performed in triplicate.

DrugUptake Inhibition at DAT
IC50 (nM)
Uptake Inhibition at NET
IC50 (nM)
Uptake Inhibition at SERT
IC50 (nM)
Mephedrone769 ± 106319 ± 40600 ± 99
4-CMC1014 ± 78559 ± 57542 ± 38
4-CEC1455 ± 1102848 ± 292589 ± 44
4-CαPPP569 ± 57764 ± 79>10,000
Release at DATRelease at NETRelease at SERT
EC50 (nM) [% Emax]aEC50 (nM) [% Emax]aEC50 (nM) [% Emax]a
Mephedrone103 ± 16 [114]83 ± 20 [100]188 ± 22 [108]
4-CMC91 ± 11 [109]99 ± 18 [102]169 ± 20 [109]
4-CECInactive3058 ± 547 [81]191 ± 26 [107]
4-CαPPPInactiveInactiveInactive
  • a% Emax is defined as percentage of maximal releasing response as described in Materials and Methods.