Tsukagoshi S, Ohta J, Taguchi T
Cancer Chemotherapy Center, Japanese Foundation for Cancer Research.
Gan To Kagaku Ryoho. 1993 Nov;20(14):2108-14.
This paper described an outline of pharmacological studies of 5-HT3 receptor antagonists, mainly on ondansetron, which control nausea and vomiting associated with cancer chemotherapy. Administration of cytotoxic drugs is known to increase serotonin (5-HT) concentrations, and when released, 5-HT provokes the emetic responses via two routes; 1) 5-HT acts as an intrinsic transmitter substance and stimulates the emetic response via 5-HT3 receptors on vagal afferent terminals; 2) 5-HT transmits impulses to the vomiting center via 5-HT3 receptors on the chemoreceptor trigger zone in the area postrema of the central nervous system. 5-HT3 receptor antagonists are thought to exert an antiemetic action by specifically and competitively blocking 5-HT3 receptors.
本文描述了5-羟色胺3（5-HT3）受体拮抗剂的药理学研究概况，主要针对控制癌症化疗相关恶心和呕吐的昂丹司琼。已知细胞毒性药物的给药会增加血清素（5-HT）浓度，并且5-HT释放后会通过两条途径引发呕吐反应：1）5-HT作为内源性递质物质，通过迷走神经传入终末上的5-HT3受体刺激呕吐反应；2）5-HT通过中枢神经系统最后区化学感受触发区上的5-HT3受体将冲动传递至呕吐中枢。5-HT3受体拮抗剂被认为通过特异性和竞争性阻断5-HT3受体发挥止吐作用。
