Palonosetron

Palonosetron Structure
CAS No.
135729-61-2
Chemical Name:
Palonosetron
Synonyms
2-Qhbiqo;Palonosetron;PALONOSETRON;Rs 25233-197;Palonosetron [inn];Palonosetron hydrochloride salt;13C,2H3]-Palonosetron hydrochloride salt;(S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one;2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one;(S-(R*,R*))-2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one
CBNumber:
CB32131051
Molecular Formula:
C19H24N2O
Molecular Weight:
296.41
MOL File:
135729-61-2.mol
Modify Date:
2023/5/21 10:59:17

Palonosetron Properties

Melting point 87-88°
alpha D -136° (c = 0.25 in chloroform)
Boiling point 470.4±45.0 °C(Predicted)
Density 1.24±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO
form Powder
pka 9.77±0.33(Predicted)

Palonosetron Chemical Properties,Uses,Production

Description

Palonosetron is a new generation 5-HT3 antagonist and It has hasgreater receptor-binding properties, which results in a much longer half-life than the previously described drugs. This selective and conformationally restricted 5-HT3 receptor antagonist was approved for the treatment of chemotherapy-induced nausea and vomiting. The drug was originally developed by Syntex Corp (now Roche Bioscience) and is currently being developed by Helsinn and MGI Pharm.

Uses

Palonosetron is a serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.

Definition

ChEBI: An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.

Enzyme inhibitor

This serotonin 5-HT3 receptor antagonist and longlasting anti-emetic (FW = 296.41 g/mol; CAS 135729-61-2), known by code name RS 25259, RS 25259-197, trade name Aloxi?, and systematic name (3aS)-2-[(3S)-1- azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin- 1-one, is used to treat chemotherapy-induced nausea/vomiting. Polonosetron affects both peripheral and central nervous systems, reducing vagus nerve activity, thereby deactivating the 5-HT3 receptor-dense vomiting center located in the medulla oblongata. It is without effect on dopamine receptors or muscarinic receptors. Primary Mode of Inhibitor Action: Intravenously administered palonosetron has a linear pharmacokinetic profile, with a long terminal elimination half-life of ~40 hours and moderate (62%) plasma protein binding. Its high affinity and long half-life most likely explains its persistent antiemetic effect. Similar 5- HT3 antagonists include tropisetron, ondansetron, dolasetron, and granisetron. The effectiveness of each depends on particular variants of 5- HT3 receptors expressed by the patient, including changes in promoters for the receptor genes

Palonosetron Preparation Products And Raw materials

Raw materials

Preparation Products

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Palonosetron [inn] Rs 25233-197 (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one (S-(R*,R*))-2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one 1H-Benz(de)isoquinolin-1-one, 2-(1-azabicyclo(2.2.2)oct-3-yl)-2,3,3A,4,5,6-hexahydro-, (S-(R*,R*))- 2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one 2-Qhbiqo PALONOSETRON Palonosetron 1H-Benz[de]isoquinolin-1-one, 2-(3S)-1-azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-, (3aS)- Palonosetron hydrochloride salt PalonosetronQ: What is Palonosetron Q: What is the CAS Number of Palonosetron Q: What is the storage condition of Palonosetron 13C,2H3]-Palonosetron hydrochloride salt 135729-61-2