SB 243213 dihydrochloride

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Cat.No. 3527 - SB 243213 dihydrochloride | C22H19F3N4O2.2HCl | CAS No. 200940-23-4
Description: Selective 5-HT2C inverse agonist
Chemical Name: 2,3-Dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-Indole-1-carboxamide dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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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


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