Stables R, Andrews P L, Bailey H E, Costall B, Gunning S J, Hawthorn J, Naylor R J, Tyers M B
Glaxo Group Research Ltd., Ware, Herts, U.K.
Cancer Treat Rev. 1987 Dec;14(3-4):333-6. doi: 10.1016/0305-7372(87)90026-0.
GR38032F is a highly selective 5HT3-receptor antagonist which inhibits vomiting induced by cisplatin, cyclophosphamide or X-radiation in the ferret. Since cisplatin selectively increased the levels of 5HT and 5HIAA in the intestinal mucosa, a possible site of the antiemetic action of GR38032F may be on 5HT3-receptors on vagal afferents in the small intestine. The potent antiemetic action of GR38032F should be of clinical value in reducing the nausea and vomiting associated with radiotherapy or chemotherapy of cancer.
GR38032F是一种高度选择性的5-羟色胺3（5HT3）受体拮抗剂，它能抑制雪貂因顺铂、环磷酰胺或X射线照射引起的呕吐。由于顺铂能选择性地提高小肠黏膜中5-羟色胺（5HT）和5-羟吲哚乙酸（5HIAA）的水平，GR38032F的止吐作用可能作用于小肠迷走传入神经上的5HT3受体。GR38032F强效的止吐作用在减轻癌症放疗或化疗相关的恶心和呕吐方面应具有临床价值。
