Ondansetron Hydrochloride Dihydrate

Catalog No.S4748 Batch:S474801

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Technical Data

Formula

C18H19N3O.HCl.2H2O
Molecular Weight 365.85 CAS No. 103639-04-9
Solubility (25°C)* In vitro DMSO 73 mg/mL (199.53 mM)
Water 73 mg/mL (199.53 mM)
Ethanol 40 mg/mL (109.33 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.
Targets
5-HT3 receptor [2]
810 nM
In vitro 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].
In vivo 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].

Protocol (from reference)

Cell Assay:[3]
  • Cell lines

    PN1A and P1(0.5) cells; PSI-2, U87MG

  • Concentrations

    10 or 30 μg/ml

  • Incubation Time

    3 days

  • Method

    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.
Animal Study:[3]
  • Animal Models

    Male adult Wistar rats

  • Dosages

    2 mg/kg

  • Administration

    i.p.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.