Home Neuronal Signaling 5-HT Receptor antagonist Ondansetron Hydrochloride Dihydrate

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Ondansetron Hydrochloride Dihydrate 5-HT Receptor antagonist

Cat.No.S4748

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 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 365.85

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Quality Control

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

Cell Culture, Treatment & Working Concentration

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
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
HEK cells Function assay Inhibition of human ERG expressed in HEK cells by patch clamp technique, IC50=0.4 μM
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.81283 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (199.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 73 mg/mL

Ethanol : 40 mg/mL

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 365.85 Formula

C18H19N3O.HCl.2H2O

 Storage (From the date of receipt)
CAS No. 103639-04-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.O.O.Cl

Mechanism of Action

Targets/IC50/Ki
5-HT3 receptor
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. 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.
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. 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.
References

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