Tropisetron: molecular mechanisms of action at the 5-HT3 receptor and the glycine receptor

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Tropisetron and related drugs are used clinically to combat chemotherapy-induced nausea and vomiting. These drugs are termed '5-HT3 antagonists' because they block the activity of 5-HT3 receptor ion channels, which are found in parts of the brain that control the vomit reflex. Tropisetron also has potent effects on the glycine receptor chloride channel, which inhibits the nervous system. Depending on the concentration used, tropisetron can either increase or decrease the activity of the glycine receptor. If a drug can be found to selectively increase glycine receptor activity, it may be useful as an analgesic. In this project, we aim to understand the molecular mechanisms by which tropisetron interacts with the 5-HT3 receptor and the glycine receptor. This may help to identify novel analgesic drugs and more selective anti-emetic drugs.