Table 2.
kτ values and ratios for AT1 angiotensin receptor-mediated arrestin recruitment, diacylglycerol production and calcium mobilization.
Ligand | Arrestin | Diacylglycerol | Calcium | |||||
---|---|---|---|---|---|---|---|---|
kτ (NFU.min−1)1 | kτ (% AngII) | kτ (NFU.min−1)1 | kτ (% AngII) | Arrestin/DAG kτ ratio (% AngII ratio) | kτ (NFU.min−1)1 | kτ (% AngII) | Arrestin/Ca2+kτ ratio (% AngII ratio) | |
AngII | 0.40 ± 0.03 | 100 | 1.7 ± 0.2 | 100 | 1.00 | 2.2 ± 0.2 | 100 | 1.0 |
TRV120055 | 0.37 ± 0.02 | 92 | 2.1 ± 0.1 | 120 | 0.74 | 2.5 ± 0.2 | 110 | 0.81 |
TRV120045 | 0.38 ± 0.06 | 93 | 0.66 ± 0.02 | 30 | 3.1 | |||
TRV120026 | 0.25 ± 0.03 | 62 | 0.46 ± 0.08 | 21 | 3.0 | |||
SII | 0.20 ± 0.04 | 49 | 0.25 ± 0.06 | 12 | 4.2 |
kτ was measured from the time course data for a maximally-stimulating concentration of ligand (32 μM) as described in Fig. 5 and Supplementary Fig. S6. For kτ normalized to AngII, the mean kτ value for the ligand was divided by that for AngII. The kτ ratio was calculated by dividing kτ normalized to AngII for arrestin by kτ normalized to AngII for the pathway (DAG or Ca2+) Data are mean ± s.e.m. from three experiments, except for SII in arrestin recruitment (n = 2). 1 NFU, normalized fluorescence units.