SB 243213 dihydrochloride

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Cat.No. 3527 - SB 243213 dihydrochloride | C22H19F3N4O2.2HCl | CAS No. 1780372-25-9
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)
Reviews
Literature (4)

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.

Technical Data

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.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.99 mL 19.95 mL 39.89 mL
2.5 mM 0.8 mL 3.99 mL 7.98 mL
5 mM 0.4 mL 1.99 mL 3.99 mL
25 mM 0.08 mL 0.4 mL 0.8 mL

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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

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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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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.

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