Palonosetron hydrochloride

Discontinued Product

7038 has been discontinued.

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说明: Highly potent and high affinity 5-HT3 antagonist
化学名: (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
纯度: ≥98% (HPLC)
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生物活性 for Palonosetron hydrochloride

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.

技术数据 for Palonosetron hydrochloride

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.

产品说明书 for Palonosetron hydrochloride

参考文献 for Palonosetron hydrochloride

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

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5-HT Receptors Scientific Review

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.