Research Area: Cancer
Biological Activity:
Y-25130 hydrochloride is a selective and potent 5-HT3 antagonist with a Ki of 2.9 nM. [1] Y-25130 hydrochloride is a hydrochloride salt form of Y-25130.Y-25130 prevents the emesis induced by the combined treatment of doxorubicin and cyclophosphamide in ferrets. The antiemetic effect of Y-25130 is more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets is very similar to that of ondansetron. In conclusion, Y-25130 is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide- induced emeses. Addtionally, Y-25130 reveals low affinity for histamine H1 receptors with an IC50 of 4.4 μM. However, Y-25130 could not reveal any affinities for the other receptors (5-HT1A, 5-HT2, dopamine D1, dopamine D2, alpha 1-adrenoceptor, alpha 2-adrenoceptor, muscarine and benzodiazepine) even at a 10 μM concentration. In the isolated rabbit heart, Y-25130 antagonizes the indirect sympathomimetic responses to 5-HT (pA2 value = 10.06). [2]References on Y-25130 HCl[1] Jpn J Pharmacol., 1993, 63(3):377-83[2] Jpn J Pharmacol., 1992, 59(4):443-8 |