SB 243213 dihydrochloride
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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
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Keywords: SB 243213 dihydrochloride, supplier, SB243213, dihydrochloride, selective, 5-ht3, inverse, agonists, serotonergics, 5-HT2C, Receptors, 5-HT2C, Receptors, Tocris Bioscience
1 Citation for SB 243213 dihydrochloride
Citations are publications that use Tocris products. Selected citations for SB 243213 dihydrochloride include:
Ward et al (2015) Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis. Nat Commun 290 12844 PMID: 25825490
Do you know of a great paper that uses SB 243213 dihydrochloride from Tocris? If so please let us know.
Literature in this Area
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.
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