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Submit ReviewSB 242084
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)
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 |
| InChI Key | GCMNSEILNIPNSX-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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:
Cicero et al (2016) A High Throughput Phenotypic Screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells. Sci Rep 6 34798 PMID: 27739443
Fouad et al (2010) Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors. J Neurophysiol 104 2975 PMID: 20861436
Canal et al (2010) The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen. Psychopharmacology (Berl) 209 163 PMID: 20165943
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
Zhang et al (2013) Serotonin receptor 2C and Ins secretion. PLoS One 8 e54250 PMID: 23349838
Manvich et al (2012) Effects of serotonin 2C receptor agonists on the behavioral and neurochemical effects of cocaine in squirrel monkeys. J Pharmacol Exp Ther 341 424 PMID: 22328576
Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217
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
300nM
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.
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.
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