pKB values for antagonists at mutant or WT receptors
Data are presented as mean ± S.E.M. The values in parentheses represent the number of individual experiments performed.
Receptor | Agonist | Antagonist | ||||
|---|---|---|---|---|---|---|
| sCT8-32 | CGRP8-37 | BIBN4096BS | ||||
| WT AMY1(a) | rAmy | 7.78 ± 0.13 (11)e | 6.62 ± 0.13 (11)e | 7.44 ± 0.2 (7) | ||
| W74A AMY1(a) | rAmy | 7.48 ± 0.33 (3) | 6.39 ± 0.48 (3) | 6.50 ± 0.16 (3)* | ||
| W74K AMY1(a) | rAmy | 7.47 ± 0.24 (5) | 6.15 ± 0.15 (5) | 5.67 ± 0.18 (5)** | ||
| WT AMY1(a) | hβCGRP | 7.68 ± 0.18 (12)e | 6.78 ± 0.13 (14)e | 7.67 ± 0.17 (12) | ||
| W74A AMY1(a) | hβCGRP | 7.28 ± 0.29 (4) | 6.25 ± 0.26 (4) | 6.24 ± 0.32 (5)†† | ||
| W74K AMY1(a) | hβCGRP | 7.86 ± 0.25 (3) | 6.23 ± 0.56 (3) | 6.25 ± 0.22 (3)†† | ||
| WT AMY3(a) | rAmy | 7.92 ± 0.19 (6)e | 6.17 ± 0.26 (7)e | ≥ 5f (11) | ||
| E74W AMY3(a) | rAmy | 8.28 ± 0.16 (4) | 5.85 ± 0.15 (4) | 5.6 ± 0.12 (4) | ||
| WT CGRP1 | hαCGRP | 7.60 ± 0.44 (4) | 10.14 ± 0.44 (3) | |||
| W74A CGRP1 | hαCGRP | 7.66 ± 0.30 (4) | 8.59 ± 0.18 (4)a | |||
| W74K CGRP1 | hαCGRP | 8.02 ± 0.25 (4) | 8.41 ± 0.24 (4)aa | |||
| WT CGRP1 | hβCGRP | 7.00 ± 0.43 (3) | 9.73 ± 0.24 (3) | |||
| W74A CGRP1 | hβCGRP | 7.26 ± 0.35 (4) | 8.45 ± 0.31 (4)bb | |||
| W74K CGRP1 | hβCGRP | 7.25 ± 0.25 (4) | 7.49 ± 0.12 (4)bb | |||
| WT AM2 | hAM | 6.51 ± 0.06 (4) | 6.39 ± 0.25 (4) | |||
| E74W AM2 | hAM | 6.14 ± 0.13 (3) | 7.56 ± 0.11 (4)cc | |||
| WT AM2 | hβCGRP | 6.02 ± 0.38 (3) | 6.29 ± 0.16 (4) | |||
| E74W AM2 | hβCGRP |
| 5.96 ± 0.23 (3) | 7.35 ± 0.19 (3)d | ||
*p < 0.05, **p < 0.01 versus WT AMY1(a) for rAmy with BIBN4096BS.
††p < 0.01 versus WT AMY1(a) for βCGRP with BIBN4096BS.
↵ a p < 0.05, aap < 0.01 verus WT CGRP1 for hαCGRP with BIBN4096BS.
↵ bb p < 0.01 versus WT CGRP1 for hβCGRP with BIBN4096BS.
↵ cc p < 0.01 versus WT AM2 for hAM with BIBN4096BS.
↵ d p < 0.05 versus WT AM2 for hβCGRP with BIBN4096BS, one-way ANOVA followed by Dunnett's multiple comparison test.
↵ e Data from Hay et al. (2005); experiments were performed in parallel with this study.
↵ f For 8 of 11 experiments, a pKB value could not be determined, but on three occasions, the pKB was equal to 5.4.