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Tropisetron HCl(SDZ-ICS-930 HCl)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tropisetron HCl(SDZ-ICS-930 HCl)图片
CAS NO:105826-92-4
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议
25g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)320.81
FormulaC17H20N2O2.HCl
CAS No.105826-92-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 35 mg/mL (109.1 mM)
Water: 46 mg/mL (143.4 mM)
Ethanol: <1 mg/mL
Other infoChemical Name: (1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 1-methyl-1H-indole-3-carboxylate hydrochloride

SMILES: O=C(C1=CN(C)C2=C1C=CC=C2)OC3C[C@@H](N4C)CC[C@H]4C3.[H]Cl

SynonymsTrade name Navoban; ICS-205930; ICS 205-930; Tropisetron; ICS 205930; ICS205930; ICS 205-930; ICS-205-930; Tropisetron HCl;
实验参考方法
In Vitro

In vitro activity: Tropisetron is a high affinity ligand for both th α7 nAChR and 5HT3R. Tropisetron has very low affinity for the other nicotinic subtypes tested. Tropisetron is a potent and selective serotonin 3 (5-hydroxytryptamine3; 5-HT3) receptor antagonist with antiemetic properties, probably mediated via antagonism of receptors both at peripheral sites and in the central nervous system. Tropisetron is a potent inhibitor of early and late events in TCR-mediated T cell activation. Tropisetron specifically inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Ttropisetron inhibits both the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation but in contrast TNF(alpha)-mediated NF-(kappa)B activation is not affected by this antagonist. Tropisetron acts on α7 nAChRs on isolated pig retinal ganglion cells (RGCs) to provide neuroprotection against glutamate-induced excitotoxicity. Tropisetron acts to decrease p38MAP kinase levels to inhibit apoptosis. Tropisetron is able to protect retinal ganglion cells (RGCs) from a glutamate assault in a dose-dependent manner when applied to cultures 1 hour prior to glutamate application.


Cell Assay: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs).

In VivoTropisetron (1 mg/kg i.p.) significantly improves the deficient inhibitory processing of the P20-N40 auditory evoked potential in DBA/2 mice.
Animal modelMice
Formulation & Dosage1 mg/kg i.p.
References

Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21; Psychopharmacology (Berl). 2005 Nov;183(1):13-9.