Table 1.
Competition Binding to the RG and R0 Conformations of the Human PTHR
| IC50 (nm)
|
|||||
|---|---|---|---|---|---|
| RG [125I]PTH(1–15) + GSND | n | R0 [125I]PTH(1–34) + GTPγS | n | R0:RG | |
| [Nle8,21,Tyr34]rPTH(1–34)NH2 | 0.91 ± 0.28 | 6 | 4.0 ± 0.6 | 6 | 4 |
| [His5,Nle8,21,Tyr34]rPTH(1–34)NH2 | 0.10 ± 0.03 | 3 | 67 ± 8 | 3 | 670 |
| [Tyr36]hPTHrP(1–36)NH2 | 0.42 ± 0.09 | 3 | 28 ± 6 | 3 | 66 |
| [Ile5,Tyr36]hPTHrP(1–36)NH2 | 0.92 ± 0.07 | 3 | 2.9 ± 0.1 | 3 | 3 |
| rPTH(1–34)NH2 | 0.34 ± 0.16 | 3 | 2.3 ± 0.3 | 3 | 7 |
| [His5]rPTH(1–34)NH2 | 0.19 ± 0.04 | 5 | 26 ± 5 | 5 | 138 |
| hPTH(1–34)NH2 | 0.39 ± 0.24 | 3 | 6.6 ± 2.4 | 3 | 17 |
| [His5]hPTH(1–34)NH2 | 0.76 ± 0.04 | 5 | 122 ± 35 | 5 | 160 |
| hPTHrP(1–36)NH2 | 0.59 ± 0.02 | 3 | 24 ± 3 | 3 | 42 |
| [Aib1,3,M]rPTH(1–15)NH2 | 0.74 ± 0.18 | 3 | 1029 ± 148 | 3 | 1397 |