5-HT3 Antagonist - Development

Development

5-HT3 receptor antagonists or serotonin antagonists were first introduced in the early 1990s, and they have become the most widely used antiemetic drugs in chemotherapy. They have also been proven safe and effective for treatment of postoperative nausea and vomiting. Serotonin (5-HT) is found widely distributed throughout the gut and the central nervous system. In the gut, 5-HT is found mostly in mucosal enterochromaffin cells. Enterochromaffin cells are sensory transducers that release 5-HT to activate intrinsic (via 5-HT1P and 5-HT4 receptors) and extrinsic (via 5-HT3 receptors) primary afferent nerves. Chemotherapeutic drugs for malignant disorders that cause vomiting have been found to cause release of large amounts of serotonin from enterochromaffin cells in the gut, serotonin acts on 5-HT3 receptors in the gut and brain stem.

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