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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 332.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3 mL||15.02 mL||30.04 mL|
|5 mM||0.6 mL||3 mL||6.01 mL|
|10 mM||0.3 mL||1.5 mL||3 mL|
|50 mM||0.06 mL||0.3 mL||0.6 mL|
References are publications that support the biological activity of the product.
Wong et al (1995) The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br.J.Pharmacol. 114 851 PMID: 7773546
Rojas et al (2010) The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo. J.Pharmacol.Exp.Ther. 335 362 PMID: 20724484
Lummis & Thompson (2013) Agonists and antagonists induce different palonosetron dissociation rates in 5-HT3A and 5-HT3AB receptors. Neuropharmacology. 73 241 PMID: 23747573
Del Cadia et al (2013) Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor. Bioorg.Med.Chem. 21 7523 PMID: 24128813
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.