Table 1.
The time taken for responses to tegaserod and to motilin receptor agonists to fade in rabbit isolated gastric antrum circular preparations, measuring their ability to facilitate cholinergically mediated contractions
| Compound | Concentration (n) (μM) | t1/2 values (min) |
|---|---|---|
| r.motilin | 0.003 (4) | 9.5±0.9 |
| 0.01 (4) | 12.0±1.2 | |
| 0.03 (5) | 12.0±1.3 | |
| 0.1(5) | 11.4±0.6 | |
| 0.3 (4) | 9.0±0 | |
| [Nle13]motilin | 0.01 (4) | 15.0±1.2 |
| 0.03 (5) | 14.4±1.1 | |
| 0.1 (4) | 12.0±1.2 | |
| 0.3 (5) | 11.4±1.5 | |
| Erythromycin | 1 (4) | 34.5±5.3 |
| 3 (5) | 24.0±5.6 | |
| 10 (3) | 23.0±8.7 | |
| Tegaserod | 0.1 (6) | 27.5±10.4 |
| 0.3 (4) | 28.5±8.9 | |
| 1 (6) | 42.5±10.6 | |
| 3 (6) | 28.0±12.3 | |
| 10 (6) | 11.5±0.9 |
Abbreviations: r.motilin, rabbit motilin.
After single application of the ligand and during continual incubation, the time taken for the maximum response to fade by 50% (t1/2) was measured. (time taken from when the drug was added).