CAS NO: | 105826-92-4 |
规格: | ≥98% |
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 |
Molecular Weight (MW) | 320.81 |
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Formula | C17H20N2O2.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 info | Chemical 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 |
Synonyms | Trade name Navoban; ICS-205930; ICS 205-930; Tropisetron; ICS 205930; ICS205930; ICS 205-930; ICS-205-930; Tropisetron HCl; |
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). |
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In Vivo | Tropisetron (1 mg/kg i.p.) significantly improves the deficient inhibitory processing of the P20-N40 auditory evoked potential in DBA/2 mice. |
Animal model | Mice |
Formulation & Dosage | 1 mg/kg i.p. |
References | Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21; Psychopharmacology (Berl). 2005 Nov;183(1):13-9. |