pKB values for antagonists in antagonizing agonist-induced stimulation of cAMP accumulation at human CT and AMY receptor phenotypes
Values are presented as mean ± S.E.M.
| Antagonist & Receptors | Agonist | pKB | n |
|---|---|---|---|
| sCT8-32 | |||
| CT(a) | hCT | 8.17 ± 0.17 | 7 |
| CT(a) | rAMY | 8.22 ± 0.26 | 7 |
| AMY1(a) | hCT | 7.95 ± 0.16 | 7 |
| AMY1(a) | rAMY | 7.78 ± 0.13 | 11 |
| AMY1(a) | hαCGRP | 7.80 ± 0.17 | 11 |
| AMY1(a) | hβCGRP | 7.68 ± 0.18 | 12 |
| AMY1(a) | Tyr0-hαCGRP | 7.61 ± 0.17 | 4 |
| AMY3(a) | hCT | 7.87 ± 0.25 | 6 |
| AMY3(a) | rAMY | 7.92 ± 0.19 | 6 |
| AC187 | |||
| CT(a) | hCT | 7.15 ± 0.23 | 7 |
| CT(a) | rAMY | 6.89 ± 0.25 | 7 |
| AMY1(a) | hCT | 7.30 ± 0.11 | 7 |
| AMY1(a) | rAMY | 8.02 ± 0.18 | 7 |
| AMY1(a) | hαCGRP | 7.86 ± 0.20 | 11 |
| AMY1(a) | hβCGRP | 7.85 ± 0.26 | 4 |
| AMY1(a) | Tyr0-hαCGRP | 7.73 ± 0.27 | 4 |
| AMY3(a) | hCT | 7.37 ± 0.33 | 6 |
| AMY3(a) | rAMY | 7.68 ± 0.22 | 5 |
| AC413 | |||
| CT(a) | hCT | 6.94 ± 0.13 | 7 |
| CT(a) | rAMY | 7.48 ± 0.17 | 7 |
| AMY1(a) | hCT | 7.11 ± 0.27 | 5 |
| AMY1(a) | rAMY | 7.92 ± 0.23 | 4 |
| AMY1(a) | hαCGRP | 7.30 ± 0.24 | 10 |
| AMY1(a) | hβCGRP | 7.25 ± 0.21 | 2 |
| AMY1(a) | Tyr0-hαCGRP | 7.44 ± 0.67 | 2 |
| AMY3(a) | hCT | 6.83 ± 0.27 | 8 |
| AMY3(a) | rAMY | 7.10 ± 0.14 | 8 |
| hαCGRP8-37 | |||
| CT(a) | hCT | <5 | 5 |
| CT(a) | rAMY | <5 | 4 |
| AMY1(a) | hCT | <5 | 7 |
| AMY1(a) | rAMY | 6.62 ± 0.13 | 11 |
| AMY1(a) | hαCGRP | 6.79 ± 0.24 | 9 |
| AMY1(a) | hβCGRP | 6.78 ± 0.13 | 14 |
| AMY1(a) | Tyr0-hαCGRP | 6.56 ± 0.4 | 6 |
| AMY3(a) | hCT | ≤5 | 8 |
| AMY3(a) | rAMY | 6.17 ± 0.26 | 7 |
| rAMY8-37 | |||
| CT(a) | hCT | <5 | 2 |
| CT(a) | rAMY | <5 | 2 |
| AMY1(a) | hCT | <5 | 4 |
| AMY1(a) | rAMY | 5.59 ± 0.24 | 3 |
| AMY1(a) | hαCGRP | N.D. | |
| AMY1(a) | hβCGRP | N.D. | |
| AMY1(a) | Tyr0-hαCGRP | N.D. | |
| AMY3(a) | hCT | <5 | 3 |
| AMY3(a) | rAMY | <5 | 4 |
| hAM22-52 | |||
| CT(a) | hCT | <5 | 1 |
| CT(a) | rAMY | <5 | 1 |
| AMY1(a) | hCT | <5 | 3 |
| AMY1(a) | rAMY | <5 | 3 |
| AMY1(a) | hαCGRP | <5 | 1 |
| AMY1(a) | hβCGRP | <5 | 1 |
| AMY1(a) | Tyr0-hαCGRP | N.D. | |
| AMY3(a) | hCT | <5 | 4 |
| AMY3(a) | rAMY | <5 | 4 |
N.D., not done; <5, antagonist caused no significant shift of the agonist concentration effect curve at concentrations of 10-5 M.