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

托烷司琼：5-HT3 受体和甘氨酸受体作用的分子机制

• 批准号: nhmrc : 301053
• 负责人: Prof Joseph Lynch
• 金额: $ 24.79万
• 依托单位国家: 澳大利亚
• 项目类别: NHMRC Project Grants
• 财政年份: 2004
• 资助国家: 澳大利亚
• 起止时间: 2004-01-01 至 2006-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/tropisetron-molecular-mechanisms-glycine-receptor/94944
• 关键词: Tropisetron; molecular; mechanisms; action; HT3

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.

托烷司琼和相关药物在临床上用于对抗化疗引起的恶心和呕吐。这些药物被称为5-HT3拮抗剂，因为它们阻断了5-HT3受体离子通道的活动，该通道存在于大脑中控制呕吐反射的部分。托烷司琼对抑制神经系统的甘氨酸受体氯通道也有很强的作用。托烷司琼可以增加或降低甘氨酸受体的活性，具体取决于使用的浓度。如果可以发现一种药物可以选择性地增加甘氨酸受体的活性，那么它可能会被用作止痛剂。在这个项目中，我们旨在了解托烷司琼与5-HT3受体和甘氨酸受体相互作用的分子机制。这可能有助于发现新的止痛药和更具选择性的止吐药物。