Table 1.
PTHR1 and PTHR2 Activation for PTH(1-34) and α/β/γ-Analogues 1 and 2.
PTHR1 cAMP Production | PTHR2 cAMP Production | |||||||
---|---|---|---|---|---|---|---|---|
Peptide | pEC50 | EC50 (nM) |
EC50 relative |
% Max | pEC50 | EC50 (nM) |
EC50 relative |
% Max |
PTH(1-34) | 9.2 ± 0.1 | 0.58 | 1 | 102 ± 4 | 9.2 ± 0.05 | 0.69 | 1 | 100 ± 2 |
1 | 8.6 ± 0.1 | 2.3 | 4 | 116 ± 6 | 7.5 ± 0.07 | 29 | 42 | 76 ± 3 |
2 | 8.2 ± 0.1 | 6.2 | 11 | 119 ± 7 | 6.6 ± 0.2 | 280 | 406 | 11 ± 2 |
For PTHR1 activation, measured via stimulation of intracellular cAMP, pEC50, EC50 and maximal response (% Max) values were derived from 4 independent experiments. For PTHR2 activation, pEC50, EC50 and % Max represent the average of ≥4 independent experiments. pEC50 indicates the negative logarithm of the half-maximal effective concentration (EC50). EC50 relative indicates cAMP potency normalized to PTH(1-34) by the quotient (α/β/γ-analogue/PTH(1-34)). pEC50 and % Max uncertainties are expressed as SEM.