Home Neuronal Signaling 5-HT Receptor antagonist - AChR 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

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

Solubility

In vitro
Batch:

Water : 56 mg/mL

DMSO : 10 mg/mL ( (35.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

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Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
5-HT3 receptor [1]
5.3 nM(Ki)
α7 nAChR [1]
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[2].
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[3].
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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