TABLE 2.

Estimated human brain concentrations of cathinones compared to the monoamine reuptake transporter and neuronal activity inhibition potencies.

Cathinones	Human (serum/blood/plasma) (μM)	Brain partitioning factor (BPF)	Estimated human (brain) (μM)	IC50 value at or close to estimated human (brain)
3-MMC	0.005–9.0A,b,c	x	0.005–9.0	hDAT > hNET
4-MMC	0.05–6.0a,d,E,f	0.7–6.21,–2,3	0.04–37	hNET > hDAT
4-MEC	0.1–4.7a,d	1.5–6.24	0.2–29	hDAT > hNET >> MSRa, MBRa, MNBRa
Methylone	0.01–18a,d,g,h	1.4–4.55,–6,7	0.01–81	hNET, hDAT >> hSERT
Pentedrone	0.04–1.9a,d,I	1.68	0.06–3.0	hDAT > hNET
α-PVP	0.01–2.8b,j,K	0.1–1.84,8,9,10	0.001–5.0	hNET > hDAT
MDPV	0.02–6.9d,L,M,n	0.8–4.44,11,12	0.02–30	hNET > hDAT >> hSERT >> MSRa, MSRp, MBRa, MNBRa

Estimated brain concentrations were calculated using human blood, serum (caps), or plasma (bold) concentrations and brain partition factors (BPF) found in literature. All human concentrations were obtained from reports on recreational use (voluntary intake, driving under the influence or accidental non-fatal intoxications). BPFs were based on blood/serum (underlined)/plasma (strikethrough) and brain concentrations of human or rat (bold) data. Estimated brain concentrations for 3-MMC were based on the observation that most BPFs are >1. Small to large differences in effect concentrations for different endpoints are depicted as > or >>, respectively. hDAT, human dopamine reuptake transporter; hNET, human norepinephrine reuptake transporter; hSERT, human serotonin reuptake transporter; MSR_a, mean spike rate during acute exposure; MBR_a, mean burst rate during acute exposure; MBNR_a, mean network burst rate during acute exposure; MSR_p, mean spike rate during prolonged exposure. References for serum concentrations: ^aTurcant et al. (2017), ^bAdamowicz et al. (2016b), ^cBackberg et al. (2015), ^dElliott and Evans (2014), ^eWood et al. (2010), ^fCosbey et al. (2013), ^gdeRoux and Dunn (2017), ^hCawrse et al. (2012), ⁱWorld Health Organisation [WHO] (2016), ^jAdamowicz et al. (2016a), ^kBeck et al. (2016), ^lKriikku et al. (2011), ^mThornton et al. (2012), ⁿMarinetti and Antonides (2013). References for BPF calculation: ¹Gerace et al. (2014), ²Hadlock et al. (2011), ³Martinez-Clemente et al. (2013), ⁴Lehmann et al. (2018), ⁵deRoux and Dunn (2017), ⁶Lõpez-Arnau et al. (2013), ⁷Štefková et al. (2017), ⁸Sykutera et al. (2015), ⁹Hasegawa et al. (2014), ¹⁰Potocka-Banas et al. (2017), ¹¹Wyman et al. (2013), ¹²Marinetti and Antonides (2013).