Palonosetron HCl

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Chemical Structure| 135729-62-3 同义名 : 帕洛诺司琼盐酸盐 ;Palonosetron (hydrochloride); RS 25259; RS 25259 197; Palonosetron HCl
CAS号 : 135729-62-3
货号 : A195751
分子式 : C19H25ClN2O
纯度 : 99%
分子量 : 332.87
MDL号 : MFCD07370072
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(9.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(300.42 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Palonosetron hydrochloride, as 5-HT3 receptor antagonist palonosetron, is an important treatment for emesis and nausea during cancer therapy. Chronic exposure to palonosetron reduced the number of available cell surface [3H]granisetron binding sites[3]. Combining low-dose palonosetron with droperidol potentiated prophylaxis for PONV (Postoperative nausea and vomiting) and achieved a similar prophylactic effect[4]. Moreover, palonosetron significantly adds to the clinician’s ability to effectively control CINV (chemotherapy-induced nausea and vomiting) in patients undergoing HEC or MEC (highly and moderately emetogenic chemotherapy)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

15.02mL

3.00mL

1.50mL

30.04mL

6.01mL

3.00mL
参考文献

[1]Gralla R, Lichinitser M, et al. Palonosetron improves prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy: results of a double-blind randomized phase III trial comparing single doses of palonosetron with ondansetron. Ann Oncol. 2003 Oct;14(10):1570-7.

[2]Wong EH, Clark R, et al. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br J Pharmacol. 1995 Feb;114(4):851-9.

[3]Hothersall JD, Moffat C, Connolly CN. Prolonged inhibition of 5-HT₃ receptors by palonosetron results from surface receptor inhibition rather than inducing receptor internalization. Br J Pharmacol. 2013 Jul;169(6):1252-62.

[4]Hu X, Tan F, Gong L. Higher dose of palonosetron versus lower dose of palonosetron plus droperidol to prevent postoperative nausea and vomiting after eye enucleation and orbital hydroxyapatite implant surgery: a randomized, double-blind trial. Drug Des Devel Ther. 2017 May 15;11:1465-1472.

[5]Celio L, Niger M, Ricchini F, Agustoni F. Palonosetron in the prevention of chemotherapy-induced nausea and vomiting: an evidence-based review of safety, efficacy, and place in therapy. Core Evid. 2015 Aug 21;10:75-87.