Biological Activity
Potent, selective 5-HT2C/2B receptor antagonist. pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 2B and 2C receptors respectively. Centrally active upon systemic administration in vivo.
Licensing Information
Sold under license
Technical Data
| M. Wt | 353.36 |
| Formula | C16H14F3N3OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 196965-14-7 |
| PubChem ID | 443389 |
| InChI Key | OQZOXHCRSXYSPM-UHFFFAOYSA-N |
| Smiles | CSC1=C(C=C2N(CCC2=C1)C(=O)NC1=CC=CN=C1)C(F)(F)F |
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 | 35.34 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 353.36. 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 | 2.83 mL | 14.15 mL | 28.3 mL |
| 5 mM | 0.57 mL | 2.83 mL | 5.66 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.83 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bristow et al (2000) Evidence for accelerated desensitisation of 5-HT2C receptors following combined treatment with fluoxetine and the 5-HT1A receptor antagonist, WAY 100,635, in the rat. Neuropharmacology 39 1222 PMID: 10760364
Bromidge et al (1998) Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. J.Med.Chem. 41 1598 PMID: 9572885
Hutson et al (2000) Activation of mesolimbic dopamine function by phencyclidine is enhanced by 5-HT2C/2B receptor antagonists: neurochemical and behavioural studies. Neuropharmacology 39 2318 PMID: 10974315
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