Table 1
Chemical structure of selected nonpeptide CGRP1 receptor antagonists
| SB-Number | Compound | Binding IC50 | Cyclase IC50 |
|---|---|---|---|
| SB-211973 |
| 1.93 ± 0.47 | 0.9 ± 0.37 |
| SB-(±)-268262 | 0.24 ± 0.03 | 0.83 ± 0.29 | |
| SB-(+)-273779 | 0.31 ± 0.04 | 0.39 ± 0.01 | |
| SB-(−)-273780 | 0.69 ± 0.19 | 2.07 ± 0.17 | |
The values represent the inhibitory concentrations obtained both in [125I]CGRP binding and CGRP-mediated adenylyl cyclase stimulation in SK-N-MC cell membranes.