TABLE 2.
Effect of antagonist with pre-incubation and a washout step on pA2 values for lipidated αCGRP8-37 analogues at hCGRP and hAMY1 receptors expressed in Cos-7 cells.
| αCGRP8-37 | αCGRP7-37-palmitate | V8C-palmitate | K24C-palmitate | K35C-palmitate | ||
|---|---|---|---|---|---|---|
| CGRPr | No washout | 9.21 ± 0.21 | 9.86 ± 0.14 | 9.85 ± 0.08 | 10.28 ± 0.12 | 6.74 ± 0.16 |
| Washout | <7.5 | 9.34 ± 0.28 a | 8.67 ± 0.20 b | 9.13 ± 0.14 c | <5.5 d | |
| AMY1r | No washout | 7.23 ± 0.10 | 9.39 ± 0.22 | 8.98 ± 0.25 | 9.43 ± 0.20 | — |
| Washout | <6 | 8.69 ± 0.27 | 8.54 ± 0.31 a | 8.45 ± 0.23 a | — | |
Values are mean ± SEM of five independent experiments. Comparisons between no washout and washout conditions were analyzed by paired Student’s t-test.
a
p < 0.05.
b
p < 0.001.
c
p < 0.01.
d
Denotes that only two out of five experiments elicited measurable pA2 values, averaging 5.60 ± 0.04.