SB 242084

Cat. No. 2901

SB 242084 C21H19ClN4O2.2HCl [1215566-78-1]

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Chemical Name: 6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride

Biological Activity

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

Technical Data

M.Wt:
467.78
Formula:
C21H19ClN4O2.2HCl
Solubility:
Soluble to 50 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
1215566-78-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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.

If you know of a relevant reference for this product please let us know.

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

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.

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.

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 insulin 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.

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.

Fouad et al (2010) Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors. J Neurophysiol 104 2975. PMID: 20861436.

Do you know of a great paper that uses SB 242084 from Tocris? If so please let us know.show all ▼show less ▲

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

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