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Submit ReviewSB 243213 dihydrochloride
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)
Biological Activity for SB 243213 dihydrochloride
SB 243213 dihydrochloride is a 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.
Technical Data for SB 243213 dihydrochloride
| M. Wt | 501.33 |
| Formula | C22H19F3N4O2.2HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1780372-25-9 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for SB 243213 dihydrochloride
References for SB 243213 dihydrochloride
References are publications that support the biological activity of the product.
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, SB 243213 dihydrochloride supplier, SB243213, dihydrochloride, selective, 5-ht3, inverse, agonists, serotonergics, 5-HT2C, Receptors, 3527, 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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.