Table 1.
Cell line | PYY |
NPY |
GTPγS |
||
---|---|---|---|---|---|
pKi | Bmax (pmol mg− 1) |
pKi | pIC50 | Inhibition (1 μM, %) |
|
sfGFP: | |||||
Y1 | 9.50 ± 0.23 | 1.5 ± 0.7 | 9.75 ± 0.16 | 9.01 ± 0.18 | 68.6 ± 6.7 |
Y16A | 9.22 ± 0.09 | 2.3 ± 0.1 | 9.69 ± 0.04 | 8.80 ± 0.21 | 72.9 ± 7.0 |
Y2 | 10.76 ± 0.09 | 2.2 ± 0.3 | 10.39 ± 0.17 | 8.81 ± 0.14 | 69.2 ± 5.4 |
Y2H155P | 10.57 ± 0.05 | 2.1 ± 0.2 | 9.91 ± 0.27 | 8.72 ± 0.15 | 46.9 ± 10.2 |
BiFC: | |||||
Y1 A1 | 9.45 ± 0.19 | 0.7 ± 0.2 | 9.58 ± 0.07 | 8.62 ± 0.26 | 68.5 ± 13.9 |
Y1 A2 | 9.54 ± 0.06 | 0.9 ± 0.4 | 9.70 ± 0.13 | 8.54 ± 0.16 | 66.7 ± 7.0 |
Y1 A2Δ | 9.44 ± 0.08 | 1.1 ± 0.3 | 9.76 ± 0.16 | 8.49 ± 0.02 | 54.9 ± 7.0 |
Y16A A1 | 9.30 ± 0.13 | 1.6 ± 0.2 | 9.76 ± 0.11 | 8.67 ± 0.12 | 69.4 ± 5.8 |
Y16A A2 | 9.48 ± 0.09 | 1.1 ± 0.3 | 9.73 ± 0.09 | 8.63 ± 0.02 | 78.2 ± 2.1 |
Data are presented as mean ± s.e.m. from 2 to 6 (typically 3) membrane competition binding experiments, using either 16 pM (Y1 receptor) or 10 pM (Y2 receptor) [125I]PYY as the radiolabel. Y1 A2Δ represents the Y1 receptor BiFC cell line incorporating the β-arrestin2 ΔLIEFD deletion mutant.