Tropisetron HCl

Catalog No.S1898 Synonyms: ICS 205-930

For research use only.

Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

Tropisetron HCl Chemical Structure

CAS No. 105826-92-4

Purity & Quality Control

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Biological Activity

Description Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.
Targets
5-HT3 [1]
In vitro

Tropisetron is a high affinity ligand for both th α7 nAChR and 5HT3R. Tropisetron has very low affinity for the other nicotinic subtypes tested. [1] 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. [2] 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. [3] 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. [4]

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. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Water 46 mg/mL
(143.38 mM)
DMSO 35 mg/mL
(109.09 mM)
Ethanol Insoluble

Chemical Information

Molecular Weight 320.81
Formula

C17H20N2O2.HCl

CAS No. 105826-92-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04195204 Recruiting Drug: Tropisetron|Drug: Placebos Postoperative Cognitive Dysfunction|Postoperative Delirium Beijing Chao Yang Hospital November 1 2020 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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