Agonist potencies (pEC50 values) for stimulation of cAMP accumulation at human CT and AMY receptors
Data are presented as mean ± S.E.M. Values in parentheses represent the number of individual experiments analyzed.
| CT(a) | AMY1(a) | AMY3(a) | |
|---|---|---|---|
| hCT | 8.99 ± 0.1 (8) | 8.93 ± 0.09 (7) | 8.02 ± 0.22 (7) |
| rAMY | 6.95 ± 0.18 (8) | 9.12 ± 0.16 (10) | 8.63 ± 0.09 (7) |
| hαCGRP | 6.80 ± 0.05 (5) | 8.70 ± 0.17 (6) | 7.60 ± 0.17 (6) |
| Tyr0-hαCGRP | <6 (2) | 7.55 ± 0.17 (7) | <6 (3) |
| hβCGRP | 7.18 ± 0.22 (2) | 9.16 ± 0.18 (9) | 7.67 ± 0.23 (6) |
| (Cys(Et)2,7)hαCGRP | <6 (3) | 7.79 ± 0.14 (5)a | <6 (6) |
| (Cys(ACM)2,7)hαCGRP | <6 (3) | 7.46 ± 0.06 (4)a | <6 (6) |
| hAM | 6.73 ± 0.45 (3) | 6.48 ± 0.28 (4) | 6.89 ± 0.51 (3) |
| IMDS | 6.53 ± 0.09 (6) | 8.07 ± 0.19 (6)b | 7.12 ± 0.19 (6) |
↵ a Note that these CGRP analogues were weak partial agonists at this receptor, with Emax values of 47.9 ± 5.4 and 22.8 ± 6% for (Cys(Et)2,7)hαCGRP and (Cys(ACM)2,7)hαCGRP, respectively. These values were generated by comparing the curve maximum asymptotes of the hαCGRP analogs with that for hαCGRP itself (set at 100%), which was used as the reference full agonist for these experiments.
↵ b Emax values for IMDS were equivalent to those of hαCGRP assayed in parallel.