Dolasetron Mesylate hydrate
(Synonyms: 甲磺酸多拉司琼,MDL-73147EF hydrate) 目录号 : GC30198A 5-HT3 receptor antagonist
Cas No.:878143-33-0
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 20 nM).1 It is selective for 5-HT3 receptors over 5-HT1A, 5-HT1B, 5-HT2, dopamine D2, α1-, α2-, β-adrenergic, M1-5 muscarinic acetylcholine, and neurokinin-1 (NK1) receptors (IC50s = >10 ?M for all).2 Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC50 = 3.8 nM).1 It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin in ferrets when administered at doses of 0.5 or 2 mg/kg.2 Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.
1.Beoijinga, P.H., Galvan, M., Baron, B.M., et al.Characterization of the novel 5-HT3 antagonists MDL 73147EF (dolasetron mesilate) and MDL 74156 in NG108-15 neuroblastoma x glioma cellsEur. J. Pharmacol.219(1)9-13(1992) 2.Miller, R.C., Galvan, M., Gittos, M.W., et al.Pharmacological properties of dolasetron, a potent and selective antagonist at 5-HT3 receptorsDrug Develop. Res.28(1)87-93(1993)
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.2806 mL | 11.4028 mL | 22.8055 mL |
5 mM | 0.4561 mL | 2.2806 mL | 4.5611 mL |
10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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