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Pharmacological properties of wild type CGRP receptor and mutants of RAMP1 and CLR.
| Receptor | CGRP | CGRP | BIBN4096BS | MK-0974 | SB-273779 |
|---|---|---|---|---|---|
| pIC50 | pEC50 | pA2 | pA2 | pA2 | |
| CGRP-WT | 8.60 ± 0.04 | 9.64 ± 0.06 | 10.63 ± 0.08 | 9.74 ± 0.09 | 7.10 ± 0.14 |
| CLR-M42A/RAMP1-WT | 8.36 ± 0.10 | 9.49 ± 0.10 | 8.95 ± 0.09∗ | 6.79 ± 0.06∗∗ | 7.08 ± 0.14 |
| CLR-WT/RAMP1-W74K | 8.33 ± 0.12 | 9.35 ± 0.15 | 8.13 ± 0.11∗ | 7.29 ± 0.09∗ | 7.11 ± 0.06 |
∗p < 0.05 and ∗∗p < 0.01, relative to same antagonist at WT receptor.
