Home Neuronal Signaling 5-HT Receptor antagonist Ondansetron Hydrochloride Dihydrate For research use only.

Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

Ondansetron Hydrochloride Dihydrate Chemical Structure

Ondansetron Hydrochloride Dihydrate Chemical Structure

CAS: 103639-04-9

Purity & Quality Control

Batch: S474801 DMSO] 73 mg/mL] false] Water] 73 mg/mL] false] Ethanol] 40 mg/mL] false Purity: 99.37%
99.37

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
MDCK2 cells Function assay Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50=0.01 μM 23241029
HEK cells Function assay Inhibition of human ERG expressed in HEK cells by patch clamp technique, IC50=0.4 μM 20889341
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.81283 μM 18448342
Click to View More Cell Line Experimental Data

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Male adult Wistar rats
Dosages 2 mg/kg
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 365.85 Formula

C18H19N3O.HCl.2H2O
CAS No. 103639-04-9 SDF Download Ondansetron Hydrochloride Dihydrate SDF
Smiles CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.O.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.53 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 73 mg/mL

Ethanol : 40 mg/mL


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