Home Neuronal Signaling 5-HT Receptor antagonist Tropisetron

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Tropisetron 5-HT Receptor antagonist

Cat.No.S5538

Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
Tropisetron 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 284.35

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Quality Control

Batch: S553801 Water]56 mg/mL]false]DMSO]10 mg/mL]false]]]false Purity: 98%
98

Solubility

In vitro
Batch:

Water : 56 mg/mL

DMSO : 10 mg/mL (35.16 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 284.35 Formula

C17H20N2O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 89565-68-4 -- Storage of Stock Solutions

Synonyms ICS 205-930 Smiles CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43

Mechanism of Action

Targets/IC50/Ki
5-HT3 receptor
5.3 nM(Ki)
α7 nAChR
6.9 nM(Ki)
In vitro
Tropisetron inhibits antigen-induced proliferation and IL-2 production in human peripheral T cells. This compound inhibits the signalling pathways that regulate the activation of the transcription factors NFAT, NF-κB and AP-1, which are known to play a critical role in the immune response.
In vivo
Tropisetron could ameliorate the ischemic brain injury via decreasing myeloperoxidase activity and TNF-α level. This compound elicits anti-inflammatory effects in experimental model of cisplatin-induced nephrotoxicity and these effects were completely 5-HT3-receptor-independent.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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