Skip to main content
. 2012 Apr 26;3(4):e13. doi: 10.1038/ctg.2012.8

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.

Table adapted from references 58,79,80,81,82,83,84,85,86 as well as company websites and FDA.gov.