Table 2.
PTHR1 β-arrestin-1 and −2 Recruitment and NLuc-PTHR1 Affinity for PTH(1-34) and α/β/γ-Analogues 1 and 2.
β-arrestin-1 Recruitment | β-arrestin-2 Recruitment | NLuc-PTHR1 Affinity | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Peptide | pEC50 | EC50 (nM) |
EC50 relative |
% Max | pEC50 | EC50 (nM) |
EC50 relative |
% Max | pIC50 | IC50 (nM) |
IC50 relative |
PTH(1-34) | 8.1 ± 0.1 | 7.2 | 1 | 101 ± 3 | 8.2 ± 0.1 | 6.8 | 1 | 101 ± 3 | 7.6 ± 0.1 | 22 | 1 |
1 | 7.0 ± 0.2 | 100 | 14 | 27 ± 3 | 7.0 ± 0.4 | 100 | 15 | 21 ± 4 | 6.9 ± 0.1 | 130 | 6 |
2 | 6.7 ± 0.3 | 190 | 26 | 39 ± 8 | 7.0 ± 0.4 | 110 | 16 | 30 ± 8 | 6.1 ± 0.1 | 720 | 33 |
For β-arrestin-1 recruitment, pEC50, EC50 and maximal response (% Max) values represent the average of ≥4 independent experiments. For β-arrestin-2 recruitment, pEC50, EC50 and % Max are the average of ≥3 independent experiments. pEC50 indicates the negative logarithm of the half-maximal effective concentration (EC50). NLuc-PTHR1 pIC50 and IC50 values are the average of 3 independent experiments. pIC50 indicates the negative logarithm of the half-maximal inhibitory concentration (IC50). EC50 and IC50 relative indicate β-arrestin-1 or −2 recruitment potency or NLuc-PTHR1 affinity normalized to PTH(1-34) by the quotient (α/β/γ-analogue/PTH(1-34)). pEC50, pIC50 and % Max uncertainties are expressed as SEM.