Tropisetron hydrochloride

Modify Date: 2025-08-24 21:29:19

Tropisetron hydrochloride Structure
Tropisetron hydrochloride structure
Common Name Tropisetron hydrochloride
CAS Number 105826-92-4 Molecular Weight 320.814
Density N/A Boiling Point 448.5ºC at 760 mmHg
Molecular Formula C17H21ClN2O2 Melting Point 283-285ºC
MSDS USA Flash Point 225ºC

 Use of Tropisetron hydrochloride


Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.IC50 value: 70.1 ± 0.9 nMTarget: 5-HT3 receptor; α7-nicotinic receptorin vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4].in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3].

 Names

Name tropisetron hydrochloride
Synonym More Synonyms

 Tropisetron hydrochloride Biological Activity

Description Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.IC50 value: 70.1 ± 0.9 nMTarget: 5-HT3 receptor; α7-nicotinic receptorin vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4].in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3].
Related Catalog
References

[1]. Rahimian R, et al. Tropisetron attenuates amyloid-beta-induced inflammatory and apoptotic responses in rats. Eur J Clin Invest. 2013 Oct;43(10):1039-51.

[2]. Swartz MM, et al. Tropisetron as a neuroprotective agent against glutamate-induced excitotoxicity and mechanisms of action. Neuropharmacology. 2013 Oct;73:111-21.

[3]. Aminian A, et al. Tropisetron diminishes demyelination and disease severity in an animal model of multiple sclerosis. Neuroscience. 2013 Jun 15;248C:299-306.

[4]. Rahimian R, et al. Tropisetron upregulates cannabinoid CB1 receptors in cerebellar granule cells: possible involvement of calcineurin. Brain Res. 2011 Oct 12;1417:1-8.

 Chemical & Physical Properties

Boiling Point 448.5ºC at 760 mmHg
Melting Point 283-285ºC
Molecular Formula C17H21ClN2O2
Molecular Weight 320.814
Flash Point 225ºC
Exact Mass 320.129150
PSA 41.90000
LogP 2.83000
Vapour Pressure 3.09E-08mmHg at 25°C
Storage condition 2-8°C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xi
RIDADR NONH for all modes of transport

 Articles5

More Articles
Determination of tropisetron in human plasma by high performance liquid chromatographic method with UV detection and its application to a bioequivalence study.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 846(1-2) , 20-3, (2007)

A simple and sensitive high performance liquid chromatography method with UV detection was described for the determination of tropisetron in human plasma. The prepared sample solution was injected ont...

Inhibition of 5-hydroxytryptamine- and enterotoxin-induced fluid secretion by 5-HT receptor antagonists in the rat jejunum.

Eur. J. Pharmacol. 248 , 157, (1993)

The effects of cholera toxin and heat stable Escherichia coli (E. coli) enterotoxin on intestinal fluid secretion are commonly considered to be mediated by cyclic nucleotides. It was demonstrated rece...

Effects of 5-hydroxytryptamine 3 receptor antagonists on gastrointestinal motor activity in conscious dogs.

J. Pharmacol. Exp. Ther. 256 , 272, (1991)

We studied the effect of 5-hydroxytryptamine 3 (5-HT3) receptor antagonists on gastrointestinal (GI) motor activity in conscious dogs with force transducers implanted chronically. During the digestive...

 Synonyms

(3-endo)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylate hydrochloride (1:1)
Tropisetron HCl
(3-endo)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylate hydrochloride
Tropisetron monohydrochloride
8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylate hydrochloride (1:1)
(3-endo)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl-1H-indol-3-carboxylathydrochlorid
1H-Indole-3-carboxylic acid, 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester, hydrochloride (1:1)
endo-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylate hydrochloride
1H-Indole-3-carboxylic acid, (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester, hydrochloride (1:1)
Navoban
MFCD02313825
Tropisetron hydrochloride
Novaban
Tropisetron (Hydrochloride)
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