IC50 values for analogs in competition for 125I-[Tyr0]hCGRPα binding to HEK 293 cells cotransfected with 100 ng of hRAMP and 100 ng of hCTR2 or hCRLR Data are presented as mean ± S.E. (n = 3).
| Competing Analogs | CTR2/RAMP1 | CTR2/RAMP2 | CTR2/RAMP3 | CRLR/RAMP1 |
|---|---|---|---|---|
| nM | ||||
| hCGRPα | 2.3 ± 0.2 | >1000 | 91.0 ± 24.8 | 4.0 ± 0.9 |
| [Tyr0]hCGRPα | 5.5 ± 0.4 | >1000 | 760 ± 379 | 5.4 ± 0.2 |
| [Cys(ACM)2,7]hCGRPα | 277 ± 29.6 | >1000 | >1000 | 124 ± 33.1 |
| [Cys(Et)2,7]hCGRPα | 59.3 ± 4.4 | >1000 | 573 ± 75.1 | 27.3 ± 4.4 |
| Rat amylin | 3.3 ± 0.4 | 52.0 ± 6.9 | 17.5 ± 4.8 | 347 ± 53.7 |