Table 1.

Effects of synthetic cathinones and comparison test drugs on transporter-mediated inhibition of uptake and stimulation of release in rat brain synaptosomes

	Mephedrone	Methylone	MDPV	MDMA	Amphetamine	Cocaine
DAT uptake IC50 (nM ± S.E.M.)	762 ± 79	1232 ± 133	4.1 ± 0.5	1009 ± 39	93 ± 17	211 ± 19
NET uptake IC50 (nM ± S.E.M.)	487 ± 66	1031 ± 162	26 ± 8	450 ± 30	67 ± 16	292 ± 34
SERT uptake IC50 (nM ± S.E.M.)	422 ± 26	1017 ± 59	3349 ± 305	125 ± 11	3418 ± 314	313 ± 17
DAT release EC50 (nM ± S.E.M.) [Emax %]	51 ± 5 [102 ± 2]	117 ± 12 [96 ± 1]	Inactive	42 ± 2 [100 ± 4]	5.8 ± 0.4 [102 ± 1]	Inactive
NET release EC50 (nM ± S.E.M.) [Emax %]	58 ± 11 [99 ± 4]	140 ± 17 [94 ± 2]	Inactive	53 ± 7 [95 ± 2]	6.6 ± 0.7 [92 ± 1]	Inactive
SERT release EC50 (nM ± S.E.M.) [Emax %]	122 ± 10 [101 ± 1]	234 ± 35[98 ± 2]	Inactive	39 ± 5 [103 ± 4]	698 ± 71 [97 ± 2]	Inactive

Uptake and release data are modified from Baumann et al. (2012b), with the exception of MDMA data, which are unpublished. Values are given as nM ± S.E.M. for N=3–4 experiments per drug. Emax % refers to percentage of maximal release response. Compounds are considered inactive in the release assay if they fail to elicit >30% of the maximal response.