MedChemExpress - Model Palonosetron hydrochloride -135729-62-3
Palonosetron hydrochloride is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition, Palonosetron hydrochloride exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron hydrochloride also possesses antidepressant activity[1][2][3][4].MCE products for research use only. We do not sell to patients.
Palonosetron hydrochloride
MCE China：Palonosetron hydrochloride
Brand：MedChemExpress (MCE)
Cat. No.HY-A0021
CAS：135729-62-3
Purity：99.96%
Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Palonosetron hydrochloride is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition, Palonosetron hydrochloride exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron hydrochloride also possesses antidepressant activity.
In Vitro：Palonosetron (10 nM, 2 hours) inhibits the enhancement effect of 5-HT on substance P (SP)-induced calcium release in NG108-15 cells, increasing the EC50 of SP from 0.62 µM to 3.7 µM[6].
In Vivo：Palonosetron (0.05 mg/kg, i.p., single dose) significantly reduces immobility in Swiss albino mice, demonstrating potential antidepressant activity[5]. alonosetron (30-300 µg/kg, i.v., single dose) dose-dependently inhibits SP-mediated neuronal responses in the Cisplatin (HY-17394)-induced rat emesis model, indicating its impact on neurotransmission[6].
IC50 & Target：5-HT3 Receptor
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References：
[1]. Barrows, et al. "A screen of FDA-approved drugs for inhibitors of Zika virus infection." Cell host & microbe 20.2 (2016): 259-270. [Content Brief]
[2]. Rojas, et al. "Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor." Anesthesia & Analgesia 107.2 (2008): 469-478. [Content Brief]
[4]. Sepúlveda-Vildósola, et al. "Palonosetron hydrochloride is an effective and safe option to prevent chemotherapy-induced nausea and vomiting in children." Archives of medical research 39.6 (2008): 601-606. [Content Brief]
[6]. Rojas C, et al. The antiemetic 5-HT3 receptor antagonist Palonosetron inhibits substance P-mediated responses in vitro and in vivo. J Pharmacol Exp Ther. 2010 Nov;335(2):362-8. [Content Brief]
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