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Ondansetron hydrochloride dihydrate

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Chemical Structure| 103639-04-9 同义名 : 昂丹司琼盐酸盐 二水合物 ;GR 38032 hydrochloride dihydrate;SN 307 hydrochloride dihydrate;Ondansetron (hydrochloride hydrate)
CAS号 : 103639-04-9
货号 : A344767
分子式 : C18H24ClN3O3
纯度 : 98%
分子量 : 365.854
MDL号 : MFCD00374371
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(287 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 15 mg/mL(41 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 52 mg/mL suspension

生物活性
靶点

  • 5-HT3

    5-HT3 receptor, IC50:810 nM

  • 5-HT3
描述 Ondansetron Hydrochloride Dihydrate is the hydrated state of Ondansetron hydrochloride. Ondansetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist as an antiemetic for cancer treatment-induced and anesthesia-related nausea and vomiting[3]. 5-HT evoked transient inward currents (EC50 = 3.4 mM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM)[4]. Indirect stimulation of nicotinic acetylcholine receptor by ondansetron can improve the auditory gating parameters of DBA/2 mice[5]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg, respectively[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.81283 μM 18448342
HEK cells Function assay Inhibition of human ERG expressed in HEK cells by patch clamp technique, IC50=0.4 μM 20889341
HEK293 cells Function assay Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by filter binding assay, Ki=0.0028 μM 21486038
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.67mL

2.73mL

1.37mL

27.33mL

5.47mL

2.73mL
参考文献

[1]Wildeboer KM, Zheng L, et al. Ondansetron results in improved auditory gating in DBA/2 mice through a cholinergic mechanism. Brain Res. 2009 Dec 1;1300:41-50.

[2]Brown AM, Hope AG, et al. Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A). J Physiol. 1998 Mar 15;507 ( Pt 3):653-65.

[3]Ye JH, Ponnudurai R, Schaefer R. Ondansetron: a selective 5-HT(3) receptor antagonist and its applications in CNS-related disorders. CNS Drug Rev. 2001 Summer;7(2):199-213. doi: 10.1111/j.1527-3458.2001.tb00195.x. PMID: 11474424; PMCID: PMC6741689.

[4]Brown AM, Hope AG, Lambert JJ, Peters JA. Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A). J Physiol. 1998 Mar 15;507 ( Pt 3)(Pt 3):653-65. doi: 10.1111/j.1469-7793.1998.653bs.x. PMID: 9508827; PMCID: PMC2230823.

[5]Wildeboer KM, Zheng L, Choo KS, Stevens KE. Ondansetron results in improved auditory gating in DBA/2 mice through a cholinergic mechanism. Brain Res. 2009 Dec 1;1300:41-50. doi: 10.1016/j.brainres.2009.08.075. Epub 2009 Sep 1. PMID: 19728991; PMCID: PMC2784252.

[6]Khedhaier A, Ben Attia M, Gadacha W, Sani M, Bouzouita K, Chouchane L, Mechkouri M, Reinberg A, Boughattas NA. Circadian rhythms in toxic effects of the serotonin antagonist ondansetron in mice. Chronobiol Int. 2003 Nov;20(6):1103-16. doi: 10.1081/cbi-120025532. PMID: 14680146.