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Submit ReviewPalonosetron 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.
分子量 | 332.87 |
公式 | C19H24N2O.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 135729-62-3 |
PubChem ID | 6918303 |
InChI Key | OLDRWYVIKMSFFB-SSPJITILSA-N |
Smiles | O=C1N([C@@H]2CN3CCC2CC3)C[C@@]4([H])CCCC5=C4C1=CC=C5.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 33.29 | 100 | |
DMSO | 3.33 | 10 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Palonosetron hydrochloride, please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.