Table 2. Clinical utility of agonists and antagonists associated with 5-HT metabolism in gastrointestinal disorders.
Target | Mechanism | Potential and documented clinical utility |
---|---|---|
5-HT1 receptor family | Agonist | FD; IBS-D |
Antagonist | FD; IBS; GERD | |
5-HT2 receptor family | Agonist | None |
Antagonist | IBS-D (women only) | |
5-HT3 receptor | Agonist | GERD; constipation-predominant IBS |
Antagonist | IBS-D; FD; nocturnal GERD; chemotherapy-induced nausea and vomiting; radiation induced nausea and vomiting; post-operative vomiting | |
5-HT4 receptor | Agonist | Chronic constipation; gastroparesis; GERD; IBS-C; IBS-M; FD |
Antagonist | GERD | |
5-HT7 receptor | Agonist | No known applications in GI disorders, however, receptor is thought to mediate colonic relaxation, therefore a potential role in functional GI disorders |
Antagonist |
Abbreviations: FD, functional dyspepsia; GI, gastrointestinal; IBS-C, constipation-predominant irritable bowel syndrome; IBS-M, mixed IBS; GERD, gastroesophageal reflux disease; IBS-D, diarrhea-predominant IBS; 5-HT, 5-hydroxytryptamine.