Selective 5-HT3 receptor antagonist and alpha-7-nicotinic receptor agonist
REVIEW Tropisetron is a highly potent and selective competitive antagonist of the 5-HT3 receptor, a subclass of serotonin receptors located on peripheral neurons and within the CNS. Surgery and treatment with certain substances, including some chemotherapeutic agents, may trigger the release of serotonin (5-HT) from enterochromaffin-like cells in the visceral mucosa and initiate the emesis reflex and its accompanying feeling of nausea. Tropisetron selectively blocks the excitation of the presynaptic 5-HT3 receptors of the peripheral neurons in this reflex, and may exert additional direct actions within the CNS on 5-HT3 receptors mediating the actions of vagal input to the area postrema.
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