Home Neuronal Signaling 5-HT Receptor antagonist Palonosetron

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Palonosetron 5-HT Receptor antagonist

Cat.No.S5740

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
Palonosetron 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 296.41

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Quality Control

Batch: S574001 DMSO]59 mg/mL]false]]]false]]]false Purity: 99%
99

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (199.04 mM)
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Chemical Information, Storage & Stability

Molecular Weight 296.41 Formula

C19H24N2O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 135729-61-2 -- Storage of Stock Solutions

Synonyms RS25259, RS 25259 197 Smiles C1CC2CN(C(=O)C3=CC=CC(=C23)C1)C4CN5CCC4CC5

Mechanism of Action

Targets/IC50/Ki
5-HT3 receptor
0.17 nM(Ki)
In vitro

This compound is a 5-HT3 receptor antagonist with a high binding affinity for this receptor and little or no affinity for other receptors.
In vivo

Palonosetron has a longer half-life and a higher binding affinity than the first-generation 5-HT3 receptor antagonists. After intravenous dosing of this compound in healthy subjects and cancer patients, an initial decline in plasma concentration is followed by a slow elimination from the body. Mean maximum plasma concentration and area under the concentration-time curves are generally dose-proportional over the dose range of 0.3 to 90 μg/kg in healthy subjects and in cancer patients. This compound has a volume of distribution of approximately 8.3 ± 2.5 L/kg and is 62% bound to plasma proteins. It is eliminated from the body through renal excretion and metabolic pathways. The mean terminal elimination half-life is approximately 40 hours.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04486157 Completed
Healthy
HK inno.N Corporation
 March 18 2021 Phase 1
NCT04466046 Completed
Postoperative Nausea and Vomiting
Daegu Catholic University Medical Center
 September 4 2019 --
NCT03148704 Unknown status
Palonosetron
Cttq
 March 8 2017 --
NCT00982995 Terminated
Nausea|Vomiting|Terminally Ill
University of Michigan Rogel Cancer Center
 November 2010 Phase 2
NCT01074697 Completed
Nausea|Vomiting|Genital Neoplasms Female
Odense University Hospital|Helsinn Healthcare SA
 April 2010 Phase 3

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