product name Tropisetron HCl
Description: Tropisetron HCl (also known as ICS 205-930) is a novel, potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy. 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.
320.81
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
Solubility (In vivo)
Synonyms
ICS 205-930
other peoduct :
| 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. Kinase Assay: Cell Assay: |
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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. |
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| References | Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21; Psychopharmacology (Berl). 2005 Nov;183(1):13-9. |
