Tyers M B
Neuropharmacology Department, Glaxo Group Research Ltd, Ware, Herts, UK.
Therapie. 1991 Nov-Dec;46(6):431-5.
5-HT3 receptors have been the focus of much research during the last decade. They are characterised by being located on neurones both peripherally and centrally; 5-HT3 agonists cause a rapid depolarisation of the membrane potential which results from the opening of cation channels; the 5-HT3 response rapidly desensitizes. 5-HT3 receptors appear to have a modulatory role on other neurotransmitters. The identification of selective agonists and antagonists for this receptor type has allowed the discovery of several important new therapeutic applications. The use of 5-HT3 receptor antagonists in psychoactive illnesses is being explored clinically. In addition, ondansetron, a selective 5-HT3 receptor antagonist, is already being used to prevent the severe nausea and vomiting caused by cancer chemotherapy and radiotherapy. The pharmacological properties of 5-HT3 antagonists are discussed in this chapter.
在过去十年中，5-羟色胺3（5-HT3）受体一直是众多研究的焦点。它们的特点是位于外周和中枢神经元上；5-HT3激动剂会导致膜电位快速去极化，这是由阳离子通道开放引起的；5-HT3反应会迅速脱敏。5-HT3受体似乎对其他神经递质具有调节作用。针对这种受体类型的选择性激动剂和拮抗剂的鉴定，使得人们发现了几种重要的新治疗应用。5-HT3受体拮抗剂在精神活性疾病中的应用正在临床研究中。此外，选择性5-HT3受体拮抗剂昂丹司琼已被用于预防癌症化疗和放疗引起的严重恶心和呕吐。本章将讨论5-HT3拮抗剂的药理特性。
