SB 242084

Pricing Availability   Qty
Description: Selective 5-HT2C antagonist; brain penetrant
Chemical Name: 6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride
Purity: ≥99% (HPLC)
Citations (10)
Reviews (1)
Literature (3)

Biological Activity for SB 242084

SB 242084 is a 5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries for SB 242084

SB 242084 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SB 242084

M. Wt 467.78
Formula C21H19ClN4O2.2HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 1049747-87-6
PubChem ID 16219981
Smiles O=C(N3C(C=C(Cl)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 for SB 242084

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 23.39 50

Preparing Stock Solutions for SB 242084

The following data is based on the product molecular weight 467.78. 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
0.5 mM 4.28 mL 21.38 mL 42.76 mL
2.5 mM 0.86 mL 4.28 mL 8.55 mL
5 mM 0.43 mL 2.14 mL 4.28 mL
25 mM 0.09 mL 0.43 mL 0.86 mL

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Product Datasheets for SB 242084

Certificate of Analysis / Product Datasheet
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References for SB 242084

References are publications that support the biological activity of the product.

Bromidge et al (1997) 6-Chloro-5-methyl-1-[[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J.Med.Chem. 40 3494 PMID: 9357513

Kennet et al (1997) SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 36 609 PMID: 9225286

Dalton et al (2006) Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology 185 45 PMID: 16470405

If you know of a relevant reference for SB 242084, please let us know.

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Keywords: SB 242084, SB 242084 supplier, Selective, 5-HT2C, antagonists, brain, penetrant, Serotonin, Receptors, SB242084, GlaxoSmithKline, GSK, 2901, Tocris Bioscience

10 Citations for SB 242084

Citations are publications that use Tocris products. Selected citations for SB 242084 include:

Krishnan (2016) Amygdala-hippocampal phospholipase D (PLD) signaling as novel mechanism of cocaine-environment maladaptive conditioned responses. Int.J.Neuropsychopharmacol. 19 1 PMID: 26802567

Ward et al (2015) Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis. Psychopharmacology (Berl) 290 12844 PMID: 25825490

Carbonaro et al (2015) The role of 5-HT2A, 5-HT 2C and mGlu2 receptors in the behavioral effects of tryptamine hallucinogens N,N-dimethyltryptamine and N,N-diisopropyltryptamine in rats and mice. Transfus Med Hemother 232 275 PMID: 24985890

Goda et al (2013) Serotonergic hallucinogens differentially modify gamma and high frequency oscillations in the rat nucleus accumbens. Psychopharmacology (Berl) 228 271 PMID: 23525524

Do you know of a great paper that uses SB 242084 from Tocris? Please let us know.

Reviews for SB 242084

Average Rating: 4 (Based on 1 Review.)

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This product is good for in vitro experiment..
By Anonymous on 06/03/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: CHO


After reaching 80% confluence, cells were treated with the selective 5-HT2CR antagonist SB242084 (300nM) or the 5-HT1BR antagonist SB216641 (1 µM), applied 10 minutes prior to agonist application.

PMID: 26802567 Reference
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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.