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Y-25130

产品号 S2018 公司名称 Selleck Chemicals
CAS号 123040-16-4 公司网站 http://www.selleckchem.com
分子式 C17H21Cl2N3O3 电 话 (877) 796-6397
分子量 386.27294 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 73242

产品价格信息

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产品别名

标题
Y-25130
IUPAC标准名
N-{1-azabicyclo[2.2.2]octan-3-yl}-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide hydrochloride
IUPAC传统名
azasetron hydrochloride

产品登记号

CAS号 123040-16-4

产品性质

作用靶点 Serotonin receptor
成盐信息 HCl
保存条件 -20°C

产品详细信息

详细说明 (English)
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

参考文献

  • Sato N, et al. Jpn J Pharmacol. 1992; 59(4):443-8.