Biological Activity
Selective 5-HT2C inverse agonist (pKb = 9.8). Displays selectivity over other 5-HT2 subtypes (pKi values are 6.8, 7.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C respectively); also exhibits >100-fold selectivity over 50 other receptors, ion channels and enzymes. Displays anxiolytic activity in rat models.
Compound Libraries
SB 243213 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 501.33 |
| Formula | C22H19F3N4O2.2HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 200940-23-4 |
| PubChem ID | 90488853 |
| InChI Key | UKMTYUXWLKQDNT-UHFFFAOYSA-N |
| Smiles | O=C(N3C(C=C(C(F)(F)F)C(C)=C4)=C4CC3)NC(C=C2)=CN=C2OC1=CC=CN=C1C.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 | 25.07 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 501.33. 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 | 1.99 mL | 9.97 mL | 19.95 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.99 mL |
| 10 mM | 0.2 mL | 1 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bromidge et al (2000) Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic a J.Med.Chem. 43 1123 PMID: 10737744
Wood et al (2001) SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolderance and withdrawal anxiety. Neuropharmacology 41 186 PMID: 11489455
Berg et al (2006) Differential effects of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxyl]-5-pyridyl]carbamoyl]-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine2C receptor-mediated responses. J.Pharmacol.Exp.Ther. 319 260 PMID: 16807362
Keywords: SB 243213 dihydrochloride, supplier, SB243213, dihydrochloride, selective, 5-ht3, inverse, agonists, serotonergics, 5-HT2C, Receptors, 5-HT2C, Receptors, Tocris Bioscience
