Serotonin (5‐hydroxytryptophan [5‐HT]) is a biologically active amine expressed in platelets, in gastrointestinal (GI) cells and, to a lesser extent, in the central nervous system (CNS). This biogenic compound acts through the activation of seven 5‐HT receptors (5‐HT_1‐7Rs). The 5‐HT₃R is a ligand‐gated ion channel belonging to the Cys‐loop receptor family. There is a wide variety of 5‐HT₃R modulators, but only receptor antagonists (known as setrons) have been used clinically for chemotherapy‐induced nausea and vomiting and irritable bowel syndrome treatment. However, since the discovery of the setrons in the mid‐1980s, a large number of studies have been published exploring new potential applications due their potency in the CNS and mild side effects. The results of these studies have revealed new potential applications, including the treatment of neuropsychiatric disorders such as schizophrenia, depression, anxiety, and drug abuse. In this review, we provide information related to therapeutic potential of 5‐HT₃R antagonists on GI and neuropsychiatric disorders. The major attention is paid to the structure, function, and pharmacology of novel 5‐HT₃R modulators developed over the past 10 years.

中文翻译：

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用于神经精神和胃肠道疾病的 5-HT3 调节剂的最新进展。

5-羟色胺（5-羟色氨酸 [5-HT]）是一种生物活性胺，在血小板、胃肠 (GI) 细胞中以及在较小程度上在中枢神经系统 (CNS) 中表达。这种生物化合物通过激活七种 5-HT 受体 (5-HT _1-7 Rs)起作用。5-HT ₃ R 是一种配体门控离子通道，属于 Cys-loop 受体家族。5-HT ₃种类繁多R 调节剂，但只有受体拮抗剂（称为 setron）已在临床上用于化疗引起的恶心和呕吐和肠易激综合征的治疗。然而，自 1980 年代中期发现 setron 以来，已经发表了大量研究，探索新的潜在应用，因为它们在中枢神经系统中的效力和轻微的副作用。这些研究的结果揭示了新的潜在应用，包括治疗精神分裂症、抑郁症、焦虑症和药物滥用等神经精神疾病。在这篇综述中，我们提供了与 5-HT ₃ R 拮抗剂对 GI 和神经精神疾病的治疗潜力相关的信息。主要关注新型 5-HT ₃的结构、功能和药理学R 调制器在过去 10 年中得到发展。