Biological Activity
Potent, orally active 5-HT3 receptor antagonist. Antiemetic. Also partial agonist of α7 nAChR.
Technical Data
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 16.04 | 50 | |
water | 32.08 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 320.82. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
Seynaeve et al (1991) 5-HT3 receptor antagonists, a new approach in emesis: a review of ondansetron, granisetron 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
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