MedChemExpress -Model Ondansetron -99614-02-5

FromMedChemExpress LLC (MCE)

Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity[1][2][3][4][5][6][7][8].

Ondansetron

MCE China：Ondansetron

Brand：MedChemExpress (MCE)

Cat. No.HY-B0002B

CAS：99614-02-5

Synonyms：GR 38032; SN 307

Purity：99.37%

Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity.

In Vivo：Ondansetron (GR 38032; SN 307) (2.4-6 mg/kg; i.p.; six times in 15 D) has TD50 with the value of 3.7±0.6 mg/kg, and LD50 of 4.6±0.5 mg/kg in mice[4]. Ondansetron (8 mg; i.p.; 1 time) with Olanzapine (HY-14541) has better effectiveness in preventing CINV in NSCLC patients, particularly for the delayed type[7]. Ondansetron (2 mg/kg; i.p.; six consecutive days) exhibits anti-inflammatory effect through 5-HT3 receptor [8].

IC50 & Target：5-HT3 Receptor

References：

[1]. Brown AM, 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. [Content Brief]

[2]. Barann M, et al. 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. [Content Brief]

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

[4]. Khedhaier A, et al. Circadian rhythms in toxic effects of the serotonin antagonist ondansetron in mice. Chronobiol Int. 2003 Nov;20(6):1103-16. [Content Brief]

[5]. Umathe SN, 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. [Content Brief]

[6]. Doggrell SA, et al. Cardiac safety concerns for ondansetron, an antiemetic commonly used for nausea linked to cancer treatment and following anaesthesia. Expert Opin Drug Saf. 2013 May;12(3):421-31. [Content Brief]

[7]. Xin Wang, et al. Effectiveness of Olanzapine Combined with Ondansetron in Prevention of Chemotherapy-Induced Nausea and Vomiting of Non-small Cell Lung Cancer. Cell Biochem Biophys. 2015 Jun;72(2):471-3. [Content Brief]

[8]. Azadeh Motavallian-Naeini, et al. Anti-inflammatory effect of ondansetron through 5-HT3 receptors on TNBS-induced colitis in rat. EXCLI J2012 Feb 22:11:30-44. eCollection 2012. [Content Brief]

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