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Updated: Jun 8, 2026

The Use of Pharmacological-challenge fMRI in Pre-clinical Research: Application to the 5-HT System
Published on: April 25, 2012
5-HT₃ antagonists under development
1Konkuk University, Bio/Molecular Informatics Center, Department of Bioscience and Biotechnology, 1 Hwayang-dong, Gwangjin-gu, Seoul 143-701, Republic of Korea.
Importance Of The Field:
The main therapeutic area of 5-HT(3) receptor antagonists is the treatment of chemotherapy-induced nausea and vomiting (CINV), which is the most common and distressing side effects of anticancer treatment. The second major clinical application of 5-HT(3) receptor antagonists is in the treatment of irritable bowel syndrome (IBS). 5-HT(3) antagonists have been widely used and found to decrease gut transit, increase fluid absorption and reduce pain. The uses of 5-HT(3) antagonists are expending to treatment of CNS diseases such as anxiety and sleep disorders as antipsychotics and so on.
Areas Covered In This Review:
The structures, in vitro activities, in vivo effects and some clinical data on 5-HT(3) receptor antagonists under development.
What The Reader Will Gain:
Future research directions in 5-HT(3) antagonists based on the clinical trial data of the pipeline molecules.
Take Home Message:
Most drug candidates in clinical trials were discovered in the early 1990s and their patent expiry is imminent. Acquiring intellectual properties of novel 5-HT(3) receptor antagonists with improved efficacies would provide a bright future. Particularly, as the current 5-HT(3) receptor antagonists are classified into only three representative structural families (one third are zacopride-like benzamides and the others are ondansteron-like tricyclic compounds and dolansetron-like bicyclic compounds), structurally diverse compound libraries need to be extensively investigated for identification of novel 5-HT(3) receptor antagonists.
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