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Ondansetron hydrochloride dihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ondansetron hydrochloride dihydrate图片
CAS NO:103639-04-9
包装与价格:
包装价格(元)
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
NSC 665799
盐酸昂丹司琼
SN 307
GR 38032
Ondansetron hydrochloride
产品介绍
Ondansetron hydrochloride 是5- HT3受体拮抗剂,可治疗化疗后的恶心和呕吐,有抗焦虑和抗精神病作用。

产品描述

Ondansetron hydrochloride 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.

体外活性

Ondansetron is a potent, highly selective, competitive antagonist at 5-HT3 receptors. It demonstrates some affinity to other receptor subtypes, including 5-HT1B, 5-HT1C, 5-HT4, opioid, and 1-adrenergic receptors, and to the μ-opioid receptor. However, ondansetron has 1000:1 selectivity toward 5-HT3 receptors[1]. Ondansetron is found to be the most potent HERG-channel blocker among several 5-HT3 antagonists, with an IC50 of 810 nM and has been reported to block Na+ channels[2].

体内活性

Ondansetron(Ond) is well tolerated and its side effects are mild. Ond acts on the CNS as well as on the peripheral nervous system (PNS). Ondansetron is available both for oral and intravenous administration. The bioavailability of orally administered ondansetron is only 60%. The low bioavailability is due to a significant first-pass metabolism. The peak plasma concentration of ondansetron is usually reached at approximately 1.5 h after oral administration. A major portion of this drug, about 75%, is bound to plasma proteins. Ondansetron is currently used to prevent and treat nausea and vomiting associated with chemotherapy, radiation treatment and general anesthesia. It has been shown to inhibit GABA and glycine receptor activity in animal models[1]. Therapeutic dose of Ond allows delivery of significantly higher amounts of Dox to the brain tissue in vivo, which is otherwise disallowed by the BBB. The rate of penetration of the blood-brain barrier by Ond is very low[3].

细胞实验

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)

Cas No.

103639-04-9

分子式

C18H24ClN3O3

分子量

365.86

别名

NSC 665799;盐酸昂丹司琼;SN 307;GR 38032;Ondansetron hydrochloride

储存和溶解度

Ethanol:38 mg/mL (103.9 mM)
H2O:67 mg/mL (183.1 mM)
DMSO:68 mg/mL (185.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years