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    Tropisetron HCl (SDZ-ICS-930 HCl)
    Tropisetron HCl (SDZ-ICS-930 HCl)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1035
    CAS #: 105826-92-4Purity ≥98%

    Description: Tropisetron HCl (Navoban; ICS-205930; ICS 205-930), the hydrochloride salt of Tropisetron which is an anti-emetic drug, is a novel, potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist that has been approved for the treatment of chemotherapy-induced nausea and vomiting. Tropisetron is a high affinity ligand for both th α7 nAChR and 5HT3R. Tropisetron has very low affinity for the other nicotinic subtypes tested.

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

    Related CAS: 89565-68-4 (free base)

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    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[[email protected]@H](N4C)CC[[email protected]]4C3.[H]Cl

    SynonymsTrade name Navoban; ICS-205930; ICS 205-930; Tropisetron; ICS 205930; ICS205930; ICS 205-930; ICS-205-930; Tropisetron HCl; 


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Tropisetron HCl
    Grand average P20–N40 waves from DBA/2 mice 20–30 min after the injection of saline (4 ml/kg i.p.), tropisetron (1 mg/kg i.p.), tropisetron + MLA (3 mg/kg i.p.), or MLA alone. Psychopharmacology (Berl). 2005 Nov;183(1):13-9. 
     
    Tropisetron HCl
    Effects of tropisetron with or without MLA on the P20–N40 test amplitudes before and after drug administration. Psychopharmacology (Berl). 2005 Nov;183(1):13-9. 
     
    Tropisetron HCl
    Effects of tropisetron with or without MLA on TC ratios before and after drug administration. Psychopharmacology (Berl). 2005 Nov;183(1):13-9. 


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