Ondansetron hydrochloride dihydrate (GR 38032) is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

5-HT3 receptor:810 nM

Ondansetron是一种高效、高选择性的竞争性5-HT3受体拮抗剂。它还对其他一些受体亚型有一定的亲和力，包括5-HT1B、5-HT1C、5-HT4、阿片类以及1-肾上腺素受体，并对μ-阿片受体有一定的亲和力。然而，ondansetron对5-HT3受体的选择性是1000:1[1]。研究发现，在多种5-HT3拮抗剂中，ondansetron是最强的HERG通道阻断剂，其IC50为810 nM，且已报告能够阻断Na+通道[2]。

Ondansetron (Ond)具有良好的耐受性，其副作用轻微。它既作用于中枢神经系统(CNS)也作用于外周神经系统(PNS)。Ondansetron 可通过口服和静脉注射给药。口服Ondansetron 的生物利用度仅为60%，这一低生物利用度由于显著的首过代谢。口服后，Ondansetron 的血浆峰值浓度通常在约1.5小时达到。约75%的该化合物与血浆蛋白结合。Ondansetron 目前用于预防和治疗化疗、放疗及全身麻醉相关的恶心和呕吐。动物模型[1]中显示，它能抑制GABA和甘氨酸受体活性。Ondansetron 的治疗剂量允许在体内向脑组织输送显著更高量的多柔比星(Dox)，而这在正常情况下会被血脑屏障(BBB)所阻止。Ondansetron 穿透血脑屏障的速率非常低[3]。

Cells are plated in 60-mm Petri dishes (2×105 per dish) and cultured in serumcontained medium for 24 h. The next day the medium is removed and serum-contained medium with or without Dox (0.1 or 0.5 μg/ml) and Ond (10 or 30 μg/ml) in combination or respectively, is added. After 3 days, the cells are washed twice with PBS, trypsinized, and counted by using the trypan blue exclusion method.(Only for Reference)