Home Neuronal Signaling 5-HT Receptor antagonist Tropisetron HCl For research use only.

Tropisetron HCl

Synonyms: ICS 205-930

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

Tropisetron HCl Chemical Structure

CAS No. 105826-92-4

Purity & Quality Control

Tropisetron HCl Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04195204 Unknown status
Postoperative Cognitive Dysfunction|Postoperative Delirium
Beijing Chao Yang Hospital
 November 1 2020 Phase 4

Chemical Information & Solubility

Molecular Weight 320.81 Formula

C17H20N2O2.HCl
CAS No. 105826-92-4 SDF Download Tropisetron HCl SDF
Smiles CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 64 mg/mL

DMSO : 35 mg/mL ( (109.09 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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