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Submit ReviewTropisetron hydrochloride
Description: Potent 5-HT3 antagonist; also α7 nAChR partial agonist
Alternative Names: Novaban,ICS 205930
Chemical Name: (3-endo)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylic acid ester monohydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Tropisetron hydrochloride
Tropisetron hydrochloride is a potent, orally active 5-HT3 receptor antagonist. Antiemetic. Also partial agonist of α7 nAChR. Activates α7Q79G-GlyR chimeric ion channels (EC50 = 38 nM)
Technical Data for Tropisetron hydrochloride
| M. Wt | 320.82 |
| Formula | C17H20N2O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 105826-92-4 |
| PubChem ID | 656664 |
| InChI Key | XIEGSJAEZIGKSA-KOQCZNHOSA-N |
| Smiles | O=C(O[C@@H]3C[C@@H]4CC[C@@H](N4C)C3)C2=CNC1=CC=CC=C12.O=C(O[C@@H]7C[C@H]8CC[C@H](N8C)C7)C6=CNC5=CC=CC=C56.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Tropisetron hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 32.08 | 100 | |
| DMSO | 16.04 | 50 |
Preparing Stock Solutions for Tropisetron hydrochloride
The following data is based on the product molecular weight 320.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.12 mL | 15.59 mL | 31.17 mL |
| 5 mM | 0.62 mL | 3.12 mL | 6.23 mL |
| 10 mM | 0.31 mL | 1.56 mL | 3.12 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets for Tropisetron hydrochloride
References for Tropisetron hydrochloride
References are publications that support the biological activity of the product.
Seynaeve et al (1991) 5-HT3 receptor antagonists, a new approach in emesis: a review of ondansetron, granis. and tropisetron. Anticancer Drugs 2 343 PMID: 1665723
Middlemiss and Tricklebank (1992) Centrally active 5-HT receptor agonists and antagonists. Neurosci.Biobehav.Rev. 16 75 PMID: 1553108
Mhatre et al (2004) 5-HT3 antagonist ICS 205-930 enhances naltrexone's effects on ethanol intake. Eur.J.Pharmacol. 491 149 PMID: 15140631
Papke et al (2004) Activity of α7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes. Bioorg.Med.Chem.Lett. 14 1849 PMID: 15050614
If you know of a relevant reference for Tropisetron hydrochloride, please let us know.
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Keywords: Tropisetron hydrochloride, Tropisetron hydrochloride supplier, Potent, 5-HT3, receptor, antagonists, orally, active, Serotonin, Receptors, ICS205930, Nicotinics, nAChRs, alpha7, a7, α7, partial, agonists, chemogenetics, Navoban, ICS, 205930, Nicotinic, (a7), PSEMs, 2459, Tocris Bioscience
4 Citations for Tropisetron hydrochloride
Citations are publications that use Tocris products. Selected citations for Tropisetron hydrochloride include:
Otvos et al (2015) Development of Plate Reader and On-Line Microfluidic Screening to Identify Ligands of the 5-Hydroxytryptamine Binding Protein in Venoms. Respir Physiol Neurobiol 7 2336 PMID: 26114334
Johnson et al (2015) Hypoxia switches episodic breathing to singlet breathing in red-eared slider turtles (Trachemys scripta) via a tropisetron-sensitive mechanism. Proc Natl Acad Sci U S A 207 48 PMID: 25543027
Spilman et al (2014) The multi-functional drug tropisetron binds APP and normalizes cognition in a murine Alzheimer's model. Brain Res 1551 25 PMID: 24389031
Sendin et al (2014) Spatiotemporal pattern of action potential firing in developing inner hair cells of the mouse cochlea. Mol Cell Biol 111 1999 PMID: 24429348
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.