Table 1.
Drugs acting via serotonergic mechanisms: sites of action and potential therapeutic areas (adapted from Spiller (2002))
| Class | Site of action | Action | Potential therapeutic use |
|---|---|---|---|
| 5HT3 antagonists | Vagal afferents | ↓Nausea | 5-HT related nausea |
| Ondansetron | Enteric interneurons | ↓Motility | Diarrhea |
| Granisetron | Secretomotor neurons | ↓Sensitivity | Visceral sensitivity |
| Alosetron | Mesenteric afferents | ↑Compliance | Dyspepsia |
| Cilansetron | |||
| 5HT4 agonists | ENS | ↑Peristalsis | Constipation |
| Tegaserod | IPANs | ↑Transit | C-IBS |
| Prucalopride | Enterocytes | ↑Secretion | Dyspepsia/gastroparesis |
| Mesenteric afferents? | ↓Sensitivity | Intestinal dysmotility | |
| Combined 5HT4 | ENS | ↑Peristalsis | Dyspepsia/gastroparesis |
| Agonist and 5HT3 | Enterocytes | ↑Transit | Intestinal dysmotility |
| Antagonist | Mesenteric afferents | ↑Secretion | C-IBS/constipation? |
| Cisapride | |||
| Mosapride | |||
| Renzapride |