SB 228357

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Description: 5-HT2C/2B antagonist/inverse agonist
Chemical Name: N-[3-Fluoro-5-(3-pyrindyl)phenyl]-2,3-dihydro-5-methoxy-6-(trifluoromethyl)-1H-indole-1-carboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for SB 228357

SB 228357 is a 5-HT2C/2B receptor antagonist (pKi values are 7.0, 8.1 and 9.1 at 5-HT2A, 2B and 2C receptors respectively). Displays inverse agonism in a 5-HT-stimulated PI hydrolysis model of 5-HT2C receptor function. Orally active in vivo.

Licensing Information

Sold under license

Technical Data for SB 228357

M. Wt 431.39
Formula C22H17F4N3O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 181629-93-6
PubChem ID 443390
InChI Key RRJLJKRFFRZRAF-UHFFFAOYSA-N
Smiles COC1=C(C=C2N(CCC2=C1)C(=O)NC1=CC(F)=CC(=C1)C1=CC=CN=C1)C(F)(F)F

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 for SB 228357

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.14 100

Preparing Stock Solutions for SB 228357

The following data is based on the product molecular weight 431.39. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.32 mL 11.59 mL 23.18 mL
5 mM 0.46 mL 2.32 mL 4.64 mL
10 mM 0.23 mL 1.16 mL 2.32 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References for SB 228357

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 ag J.Med.Chem. 43 1123 PMID: 10737744

Reavill et al (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br.J.Pharmacol. 126 572 PMID: 10188965


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Keywords: SB 228357, SB 228357 supplier, 5-HT2C, 5-HT2B, antagonists, inverse, agonists, Serotonin, Receptors, SB228357, 1375, Tocris Bioscience

Citations for SB 228357

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Reviews for SB 228357

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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

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

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 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.