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Ondansetron

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Chemical Structure| 99614-02-5 同义名 : 恩丹西酮 ;SN 307;GR 38032;NSC 665799;GR 38032F;Ondansetron (hydrochloride) (CRM)
CAS号 : 99614-02-5
货号 : A150812
分子式 : C18H19N3O
纯度 : 99%
分子量 : 293.363
MDL号 : MFCD00833882
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(30.68 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
动物实验配方：
生物活性
靶点

  • 5-HT3
描述 Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[3]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 mM) signal by 70% and at 3 nM it abolished the response[4]. Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating[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, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg[6]. Ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection[7]. Ondansetron has shown good efficacy in the prevention of acute nausea and vomiting in children receiving moderately or highly emetogenic chemotherapy and/or irradiation, particularly when combined with dexamethasone[8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02436798 - Recruiting January 2019 Canada, British Columbia ... 展开 >> Children's and Women's Health Centre of British Columbia Recruiting Vancouver, British Columbia, Canada, V6H 3V4 Contact: Bruce Carleton, PharmD.    604-875-2179    bcarleton@popi.ubc.ca    Principal Investigator: Bruce Carleton, PharmD. 收起 <<
NCT01640340 Malignant Neoplasm Not Applicable Completed - United States, Ohio ... 展开 >> Ohio State University Medical Center Columbus, Ohio, United States, 43210 收起 <<
NCT00967499 Postoperative Nausea and Vomit... 展开 >>ing 收起 << Phase 2 Completed - United States, Arizona ... 展开 >> Precision Trials Phoenix, Arizona, United States, 85032 United States, California Accurate Clinical Trials, Inc Laguna Hills, California, United States, 92653 University of California San Francisco San Francisco, California, United States, 94115 United States, Florida University of Miami Miami, Florida, United States, 33136 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Ohio State University Medical Center Columbus, Ohio, United States, 43210 United States, Texas Scott and White Hospital Temple, Texas, United States, 76508 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.04mL

3.41mL

1.70mL

34.09mL

6.82mL

3.41mL
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. doi: 10.1016/j.brainres.2009.08.075.

[2]Umathe SN, Bhutada PS, et al. The 5-HT3 receptor antagonist, ondansetron, blocks the development and expression of ethanol-induced locomotor sensitization in mice. Behav Pharmacol. 2009 Feb;20(1):78-83.

[3]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

[4]Barann M, Meder W, Dorner Z, Brüss M, Bönisch H, Göthert M, Urban BW. Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects. Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):255-65

[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

[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

[7]Umathe SN, Bhutada PS, Raut VS, Jain NS, Mundhada YR. The 5-HT3 receptor antagonist, ondansetron, blocks the development and expression of ethanol-induced locomotor sensitization in mice. Behav Pharmacol. 2009 Feb;20(1):78-83.

[8]Culy CR, Bhana N, Plosker GL. Ondansetron: a review of its use as an antiemetic in children. Paediatr Drugs. 2001;3(6):441-79