Table 2.
The mean potency (pEC50) and IA values determined in cAMP accumulation assays for guinea-pig 5-HT4 and the human 5-HT4(b) receptors expressed in HEK293 cells and in the guinea-pig isolated colon LMMP preparation
| Compound |
gp 5-HT4 /HEK293 – clone 1 |
gp 5-HT4/HEK293 – clone 2 |
h 5-HT (4b) /HEK293 |
gp isolated LMMP |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| PEC50 | IA | n | pEC50 | IA | n | pEC50 | IA | n | pEC50 | IA | n | |
| mean±s.e.m. | mean (95% CI) | Mean±s.e.m. | mean (95% CI) | Mean±s.e.m. | mean (95% CI) | Mean±s.e.m. | mean (95% CI) | |||||
| Tegaserod | 8.4±0.1 | 106 (99–111) | 11 | 9.4±0.1 | 95 (99–111) | 5 | 8.7±0.1 | 127 (107–135) | 6 | 8.2±0.1 | 66 (61–72) | 3 |
| Prucalopride | 7.9±0.1 | 66 (25–107) | 3 | ND | ND | 8.2±0.1 | 95 (88–102) | 6 | 7.5±0.1 | 93 (87–100) | 14 | |
| 5-HT | 7.9±0.1 | 100 | 11 | 9.0±0.1 | 100 | 5 | 8.4±0.1 | 100 | 6 | 8.0±0.1 | 98 (94–102) | 20 |
| Cisapride | 6.9±0.1 | 76 (63–89) | 11 | 8.0±0.1 | 121 (104–138) | 5 | 7.3±0.1 | 102 (92–107) | 6 | 7.0±0.1 | 74 (69–80) | 10 |
| Mosapride | 6.3±0.1 | 22 (15–30) | 11 | 7.1±0.1 | 105 (85–125) | 5 | 6.7±0.1 | 35 (24–47) | 6 | 5.4±0.1 | 37 (32–42) | 3 |
| Metoclopramide | 5.9±0.2 | 24 (15–32) | 6 | 7.0±0.2 | 90 (78–102) | 5 | 5.9±0.1 | 39 (0–78) | 3 | 5.5±0.1 | 84 (76–92) | 8 |
Abbreviations: CI, confidence interval; 5-HT, 5-hydroxytryptamine; HEK293, human embryonic kidney 293; IA, intrinsic activity; LMMP, longitudinal muscle myenteric plexus; ND, not determined.
Values represent mean±s.e.m. or 95% CI and the number of individual experiments.