Palonosetron hydrochloride
Chemical 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 hydrochloride
Purity: ≥98%
Biological Activity
Palonosetron hydrochloride is a highly potent and high affinity 5-HT3 antagonist (IC50 = 0.24 nM for 5-HT3A; pKi = 10.4). Displays a slow dissociation rate. Inhibits 5-HT-induced enhancement of cellular response to substance P (Cat. No. 1156) in vitro. Inhibits cisplatin (Cat. No. 2251)-induced enhancement of substance P response in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro.
Wong et al.
Br.J.Pharmacol., 1995;114:851 -
The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo.
Rojas et al.
J.Pharmacol.Exp.Ther., 2010;335:362 -
Agonists and antagonists induce different palonosetron dissociation rates in 5-HT3A and 5-HT3AB receptors.
Lummis & Thompson
Neuropharmacology., 2013;73:241 -
Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.
Del Cadia et al.
Bioorg.Med.Chem., 2013;21:7523
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