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Chemical Structure| 105826-92-4 Chemical Structure| 105826-92-4

Structure of Tropisetron HCl
CAS No.: 105826-92-4

Chemical Structure| 105826-92-4

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Tropisetron HCl is a selective and competitive 5-HT3 receptor antagonist.

Synonyms: SDZ-ICS-930; Tropisetron(hydrochloride); ICS 205-930

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Product Details of Tropisetron HCl

CAS No. :105826-92-4
Formula : C17H21ClN2O2
M.W : 320.81
SMILES Code : O=C(C1=CNC2=C1C=CC=C2)O[C@@H]3C[C@@H](N4C)CC[C@@H]4C3.[H]Cl
Synonyms :
SDZ-ICS-930; Tropisetron(hydrochloride); ICS 205-930
MDL No. :MFCD02313825
InChI Key :XIEGSJAEZIGKSA-KOQCZNHOSA-N
Pubchem ID :656664

Safety of Tropisetron HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Adult pig retinal ganglion cells (RGCs) 100 nM 1 hour To investigate the neuroprotective role of tropisetron against glutamate-induced excitotoxicity. Results showed that pretreatment with 100 nM tropisetron significantly increased RGC survival to an average of 105% compared to controls. Neuropharmacology. 2013 Oct;73:111-21

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male Sprague-Dawley rats Conditioned taste aversion model Intraperitoneally (IP) 0, 0.056, 0.18, and 0.56 mg/kg Four complete cycles Assessed the aversive effects of tropisetron alone, finding that the high dose (0.56 mg/kg) induced a significant CTA after multiple conditioning trials Pharmacol Biochem Behav. 2013 Apr;105:112-7
Guinea pig Guinea pig ileal myenteric plexus Perfusion 0.1 μM Not specified The 5-HT3 receptor antagonist tropisetron did not affect anti-HuD antibody-induced nerve activation Sci Rep. 2016 Dec 1;6:38216
Wistar rats Type 2 diabetes mellitus models Intraperitoneal injection 1 and 2 mg/kg Once daily for 15 days Modulated glucose and lipid homeostasis, decreased serum levels of glucose, fructosamine, insulin resistance, triglycerides, total cholesterol, free fatty acid, and receptor for advanced glycation end products, while elevated levels of insulin, serotonin, and β-cell function RSC Adv. 2018 Mar 27;8(22):11908-11920
Male Sprague Dawley rats Cocaine self-administration model Intraperitoneal injection 1.0 or 3.0 mg/kg Single dose, 15 minutes before testing Tropisetron restored control over compulsive cocaine seeking, indicating that 5-HT3/α7-nicotinic receptors may be potential therapeutic targets for relieving compulsive drug seeking. Int J Neuropsychopharmacol. 2019 Sep 1;22(9):574-584
Wistar rats STZ-induced diabetic rat model Intraperitoneal injection 3 mg/kg Once daily for 2 weeks Tropisetron ameliorated renal damage due to diabetic nephropathy possibly by suppressing oxidative stress and alteration of SIRT1, FOXO3a, and claudin-1 levels Cell Stress Chaperones. 2021 Jan;26(1):217-227
Sprague-Dawley rats Pilocarpine-induced epileptic rat model Intraperitoneal injection 3 mg/kg/day Once daily for 3 weeks Tropisetron significantly reduced spontaneous recurrent seizures (SRS), improved cognitive function, alleviated hippocampal sclerosis, and concurrently suppressed synaptic remodeling and the m6A modification of cofilin-1 in TLE rats. Furthermore, tropisetron lowered glutamate levels without affecting GABA levels, reduced neuroinflammation, and increased ACh levels and α7nAChR expression in the hippocampi of TLE rats. CNS Neurosci Ther. 2024 Oct;30(10):e70086

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.59mL

3.12mL

1.56mL

31.17mL

6.23mL

3.12mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

[1]Macor JE, Gurley D, et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21.

[2]Lee CR, Plosker GL, McTavish D. Tropisetron. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential as an antiemetic. Drugs. 1993 Nov;46(5):925-43.

[3]Liu FC, Yu HP, Hwang TL, Tsai YF. Protective effect of tropisetron on rodent hepatic injury after trauma-hemorrhagic shock through P38 MAPK-dependent hemeoxygenase-1 expression. PLoS One. 2012;7(12):e53203. doi: 10.1371/journal.pone.0053203. Epub 2012 Dec 28. PMID: 23285267; PMCID: PMC3532400.

[4]Johnson SM, Krisp AR, Bartman ME. Hypoxia switches episodic breathing to singlet breathing in red-eared slider turtles (Trachemys scripta) via a tropisetron-sensitive mechanism. Respir Physiol Neurobiol. 2015 Feb 1;207:48-57. doi: 10.1016/j.resp.2014.12.015. Epub 2014 Dec 24. PMID: 25543027; PMCID: PMC4297688.

[5]Swartz MM, Linn DM, Linn CL. Tropisetron as a neuroprotective agent against glutamate-induced excitotoxicity and mechanisms of action. Neuropharmacology. 2013 Oct;73:111-21. doi: 10.1016/j.neuropharm.2013.05.020. Epub 2013 May 29. PMID: 23727438; PMCID: PMC3766469.

[6]Liu FC, Lee HC, Liao CC, Li AH, Yu HP. Tropisetron Protects Against Acetaminophen-Induced Liver Injury via Suppressing Hepatic Oxidative Stress and Modulating the Activation of JNK/ERK MAPK Pathways. Biomed Res Int. 2016;2016:1952947. doi: 10.1155/2016/1952947. Epub 2016 Nov 7. PMID: 27891510; PMCID: PMC5116490.

 

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