Related Experiment Video
Updated: Aug 17, 2026

High-throughput Measurement of Gut Transit Time Using Larval Zebrafish
Published on: October 23, 2018
Characterization of the metabolites of alosetron in experimental animals and human
I M Ismail1, P D Andrew, J Cholerton
1DMPK, GlaxoSmithKline Research and Development, Ware, UK. i.m.ismail@blueyonder.co.uk
Abstract:
The metabolism of radiolabelled alosetron was studied in rat, dog, rabbit, mouse and human. The metabolism in rat and dog was studied at a low and an elevated dose designed to generate sufficient quantities of metabolite for definitive identification. A strategy for the characterization of metabolites in cases of extensive metabolism was developed and demonstrated for alosetron. Semi-preparative high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometry (LC-MS), nuclear magnetic resonance (NMR) and liquid chromatography-nuclear magnetic resonance (HPLC-NMR) enabled the isolation and characterization of 28 metabolites of alosetron. The characterization of the metabolites in animal excreta facilitated the identification of human systemic metabolites.
Related Concept Videos
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
Toxicity Testing in Animals
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
Drugs for Treatment of Diarrhea-Predominant IBS
Two specific drugs used in the treatment are alosetron (Lotronex) and eluxadoline (Viberzi). Alosetron, a 5-HT3 antagonist, works by slowing the movement of stools in the gut, reducing bowel...

