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. Author manuscript; available in PMC: 2022 Jun 2.
Published in final edited form as: ACS Chem Neurosci. 2021 May 11;12(11):1873–1884. doi: 10.1021/acschemneuro.0c00712

Table 1.

Arrestin recruitment: requirement for overexpressed GRK2

Receptor Arrestin Recruitment
+ GRK2a No GRK2
−LogEC50 Emax
(% of WT+GRK2)
−LogEC50 Emax
(% of WT+GRK2)
D2L-WT 7.69 ± 0.05 100 ± 2 6.85 ± 0.05††† 59 ± 4†††
D2L-I212F 8.06 ± 0.03** 56 ± 1*** (−44%) 7.22 ± 0.08**,††† 16 ± 1***,††† (−73%)
D2S-WT 7.83 ± 0.01 100 ± 3 7.20 ± 0.13††† 59 ± 2†††
D2S-I212F 8.24 ± 0.04** 73 ± 2*** (−27%) 7.59 ± 0.09*,††† 21 ± 0.4***,††† (−66%)

Quinpirole potency is shown as −logEC50. Emax was calculated by subtracting basal response from maximal response at 10 min after adding the substrate coelenterazine h, and is shown as the percentage of D2-WT with added GRK2. For D2-I212F, the percent reduction compared to the corresponding D2-WT Emax is included in parentheses. N = 3–4 independent experiments for each condition. Data are presented as mean ± SEM.

a

From the dataset described in van der Weijden et al. (8), except after 10 min instead of 20 min of agonist stimulation. Statistical differences were calculated by 2-way ANOVA followed by Turkey’s post-hoc test (*p<0.05, **p<0.01, ***p<0.001 compared to D2-WT; †††p<0.001 compared to the corresponding +GRK2 condition).