Table 2.
EC50 (nM) | EMax (%) | |||||
---|---|---|---|---|---|---|
p versus | p versus | |||||
PTH(1‐34) | PTHrP(1‐36) | PTH(1‐34) | PTHrP(1‐36) | |||
PTH(1‐34) | 1.4 ± 0.6 | 1.00 | 0.55 | 100 ± 0 | 1.00 | 0.81 |
PTHrP(1‐36) | 1.82 ± 0.45 | 0.55 | 1.00 | 99 ± 3 | 0.81 | 1.00 |
M‐PTH(1‐11)/PTHrP(12‐36) | 4.46 ± 1.27 | 0.088 | 0.13 | 103 ± 3 | 0.46 | 0.46 |
M‐PTH(1‐14)/PTHrP(15‐36) | 5.18 ± 1.07 | 0.029 | 0.044 | 105 ± 4 | 0.37 | 0.36 |
M‐PTH(1‐17)/PTHrP(18‐36) | 6.78 ± 1.98 | 0.067 | 0.084 | 105 ± 5 | 0.36 | 0.34 |
M‐PTH(1‐18)/PTHrP(19‐36) | 6.01 ± 1.59 | 0.055 | 0.073 | 107 ± 5 | 0.28 | 0.26 |
M‐PTH(1‐22)/PTHrP(23‐36) | 2.58 ± 0.26 | 0.12 | 0.20 | 104 ± 4 | 0.39 | 0.37 |
M‐PTH(1‐26)/PTHrP(27‐36) | 1.79 ± 0.41 | 0.56 | 0.97 | 106 ± 5 | 0.38 | 0.35 |
M‐PTH(1‐30)/PTHrP(31‐36) | 1.52 ± 0.14 | 0.81 | 0.56 | 106 ± 4 | 0.21 | 0.21 |
EC50 values are peptide concentrations that stimulated 50% of the maximum response (EMax) for that peptide. Data were derived from the area‐under‐the‐curves (AUC) of time‐course luminescence responses measured at multiple doses and calculated as a % of the maximum AUC response attained in each assay with PTH(1‐34), the average of which was 104 ± 19 × 105 counts per second (cps) • min, and the corresponding basal value (not subtracted) was 0.52 ± 0.13 × 10 ^ cps • min. Data are means ± SEM of four experiments; p values determined by Student's t test compare responses to PTH(1‐34) and PTHrP(1‐36).
cAMP responses were measured in GP‐2.3 cells (HEK293 cells stably transfected to express the hPTHR1 and GloSensor cAMP reporter).