CAS 105826-92-4|Tropisetron hydrochloride
| Common Name | Tropisetron hydrochloride | ||
|---|---|---|---|
| CAS Number | 105826-92-4 | Molecular Weight | 320.814 |
| Density | / | Boiling Point | 448.5ºC at 760 mmHg |
| Molecular Formula | C17H21ClN2O2 | Melting Point | 283-285ºC |
| MSDS | USA | Flash Point | 225ºC |
Names
| Name | tropisetron hydrochloride |
|---|---|
| Synonym | More Synonyms |
Tropisetron hydrochloride BiologicalActivity
| 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 | Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease |
| 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 |
| InChIKey | XIEGSJAEZIGKSA-KOQCZNHOSA-N |
| SMILES | CN1C2CCC1CC(OC(=O)c1c[nH]c3ccccc13)C2.Cl |
| 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) |
