Table 1.

In vitro dopamine and serotonin uptake transporter inhibition (IC₅₀ values) and release data (EC₅₀ values).

Compound	Monoamine Uptake Transporter Inhibition (IC50)				Monoamine Release (EC50)
	DAT	SERT	DAT/SERT Ratio	Ref.	DAT	SERT	DAT/SERT Ratio	Ref.
Cathinone	14.0 (10–20) *	>100 *	>10 *	[9]	5.64 (3.0–10) *	>100 *	na	[9]
Methcathinone	1.12 (0.83–1.5) *	>10 *	>10 *	[9]	2.36 (1.7–3.3) *	>33 *	na	[9]
	2.4 (1.7–3.4) *	46 (30–71) *	19 (8.8–42) *	[64]	12.5 **	3.860 **	309 **	[56]
Mephedrone	3.31 (2.6–4.2) *	4.64 (3.7–5.9) *	1.4 (0.9–2.4) *	[9]	3.75 (1.7–8.4) *	5.98 (3.2–11) *	na	[9]
	1.4 (1.2–1.4) *	83 (66–104)	na	[65]	49.1 ± 8.32 **	118.3 ± 25.9 **	2.41 **	[10]
	5.7 (4.5–7.2) *	3.6 (2.8–4.6) *	0.63 (0.39–1.02) *	[66]
	970 ± 50 **	310 ± 80 **	na	[7]
	762 ± 79 **	422 ± 26 **	na	[10]	51 ± 5 **	122 ± 10 **	na	[10]
Buphedrone	4.24 (3.3–5.5) *	70 (2–2700) *	>10 *	[67]
Pentedrone	2.5 (2.0–3.2) *	135 (5–3700) *	>10 *	[67]	>100 *	>100 *	na	[55]
	0.4 (0.3–0.4) *	16 (14–18) *	na	[65]
Methedrone	35 (15–79) *	4.73(3.2–6.9) *	0.14 (0.04–0.46) *	[67]	506 **	120 **	0.24 **	[56]
Flephedrone	6.35 (4.2–9.5) *	>10 *	5.8 (0.8–41) *	[9]	12.5 (5.7–28) *	>33 *	na	[9]
					83.4 **	1290 **	15.4 **	[56]
3–FMC	1.7 (1.0–3.0) *	56 (7–472) *	>10 *	[67]
Pyrovalone	0.035 (0.03–0.04) *	13.0 (10.8–15.8) *	>100 *	[9]
α-PVP	0.2 (0.1–0.3) *	237 (196–291) *	na	[65]	>100 *	>100 *	na	[55]
	0.04 (0.01–0.1) *	>100 *	>1000 *	[64]
	12.8 **	>10,000 **	>781**	[56]
α-PPP	0.540 ± 0.076 *	188 ± 12 *	na	[55]	>10	>10	na	[55]
	196 **	>10,000 **	>51 **	[56]
α-PVT	0.342 ± 0.0049 *	242 ± 41 *	na	[55]
3,4-DMMC	9.4 (7.6–11.7) *	1.1 (0.9–1.4) *	0.12 (0.08–0.18) *	[66]
Methylone	4.82 (3.8–6.1) *	15.5 (10–26) *	3.3 (1.5–6.8) *	[9]	>100 *	>10 *	na	[9]
	2.0 (1.7–2.3) *	68 (58–80) *	na	[65]	133.0 ± 11.2 **	242.1 ± 48.3 **	1.82 **	[8]
	560 ± 50 **	230 ± 30 **	na	[11]
	12320 ± 133 **	1017 ± 59 **	na	[10]	117 ± 12 **	234 ± 35 **	na	[10]
Ethylone	5.68 (4.9–6.5) *	4.46 (3.8–5.2) *	0.8 (0.6–1.1) *	[9]	>100 *	9.9 (2.4–40) *	na	[9]
					>10 *	1.48 ± 0.25 *	na	[55]
Butylone	2.9 (2.5–3.4) *	6.22 (4.3–9.0) *	2.1 (1.3–3.6) *	[9]	>100 *	5.5 (1.8–17) *	na	[9]
	1710 ± 320 **	680 ± 130 **	na	[11]
	400 ± 20 **	1430 ± 16 **	na	[68]	(−) **	330 ± 40 **	na	[68]
Pentylone	1.34 (1.0–1.7) *	8.37 (5.4–13) *	6.2 (3.2–13) *	[67]	>100 *	>100 *	na	[55]
	120 ± 10 **	1360 ± 100 **	na	[68]	(−) **	1030 ± 180 **	na	[68]
MDPBP	0.11 (0.07–0.16) *	15 (5.4–39) *	132 (34–557) *	[64]	>10 *	>10 *	na	[55]
MDPP	1.08 ± 0.1 *	126 ± 36 *	na	[69]	>10 *	>10 *	na	[55]
	0.53 (0.27–1.1) *	75 (49–114) *	141 (45–422) *	[64]
MDPV	0.031 (0.03–0.04) *	9.3 (6.8–12.8) *	>100 *	[9]	>100 *	>100 *	na	[9]
	0.07 (0.07–0.08) *	4.5 (4.0–5.2) *	na	[65]
	0.05 (0.04–0.06) *	9.6 (3.4–27) *	192 (57–675) *	[64]
	4.1 ± 0.5 **	3305 ± 305 **	na	[10]	2.3 ± 0.8 **	(−) **	na	[10]

3-FMC = 3-Fluoromethcathinone; DAT = dopamine transporter; SERT = serotonin transporter; (−) = inactive; na = not reported by authors; DAT/SERT ratio = (DAT IC₅₀)⁻¹/(SERT IC₅₀)⁻¹, DAT/SERT ratio = (DAT EC₅₀)⁻¹/(SERT EC₅₀)⁻¹; values are expressed as mean or means ± SD, similar to original articles. The ability of tested drugs to inhibit the transport-mediated uptake is expressed as IC₅₀. The ability of tested drugs to influence the transporter-mediated release is expressed as EC₅₀. * in vitro studies for neurotransmitter reuptake inhibition and release using HEK293 (Human Embryonic Kidney 293) cell line expressing DAT and SERT (IC₅₀ and EC₅₀ values are expressed in μM). ** in vitro studies for neurotransmitter reuptake inhibition and release from rat brain synaptosomes (IC₅₀ and EC₅₀ values are expressed in nM).