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. 2017 Mar 10;7:44201. doi: 10.1038/srep44201

Table 2. Intrinsic activities and potencies of the five most active VS hits determined at the dopamine receptor subtype D2S by measuring the inhibition of forskolin-stimulated cAMP accumulation and recruitment of β-arrestin-2 after stimulation of the D2S receptor expressed in HEK cellsa.

Compound Inhibition of forskolin-stimulated cAMP accumulation
β-Arrestin recruitmentb
EC50 (nM) Emax (%)c EC50 (nM) Emax (%)d
Delphinidin N/A 20% at 100 μM N/A <7
Fumigaclavine A 250 27 N/A <7
Hordenine 3700 76 N/A <7
Salsolinol 630 21 N/A <7
Robenidine N/A <5 N/A <7
Dopamine 0.97 100 420 96

aEC50 and Emax values were derived from mean curves based on 3–7 individual dose-response curves.

bD2S-mediated recruitment of β-arrestin-2 determined with the PathHunter assay.

cMaximum effect of forskolin-stimulated cAMP inhibition relative to the effect of quinpirole.

dMaximum effect of D2S-mediated β-arrestin recruitment relative to the maximum effect of quinpirole. N/A: EC50 values could not be analysed because of low corresponding Emax values.