SB 242084
Chemical Name: 6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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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.
Bromidge et al.
J.Med.Chem., 1997;40:3494 -
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Kennet et al.
Neuropharmacology, 1997;36:609 -
Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse.
Dalton et al.
Psychopharmacology, 2006;185:45
Product Datasheets
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Citations for SB 242084
The citations listed below are publications that use Tocris products. Selected citations for SB 242084 include:
10 Citations: Showing 1 - 10
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Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers.
Authors: Moutkine Et al.
J Biol Chem 2017;292:6352
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A High Throughput Phenotypic Screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells.
Authors: Cicero Et al.
Sci Rep 2016;6:34798
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Amygdala-hippocampal phospholipase D (PLD) signaling as novel mechanism of cocaine-environment maladaptive conditioned responses.
Authors: Krishnan
Int.J.Neuropsychopharmacol. 2016;19:1
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Regulation of oligomeric organization of the serotonin 5-hydroxytryptamine 2C (5-HT2C) receptor observed by spatial intensity distribution analysis.
Authors: Ward Et al.
Psychopharmacology (Berl) 2015;290:12844
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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.
Authors: Carbonaro Et al.
Transfus Med Hemother 2015;232:275
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Serotonin receptor 2C and Ins secretion.
Authors: Zhang Et al.
PLoS One 2013;8:e54250
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Serotonergic hallucinogens differentially modify gamma and high frequency oscillations in the rat nucleus accumbens.
Authors: Goda Et al.
Psychopharmacology (Berl) 2013;228:271
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Effects of serotonin 2C receptor agonists on the behavioral and neurochemical effects of cocaine in squirrel monkeys.
Authors: Manvich Et al.
J Pharmacol Exp Ther 2012;341:424
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The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen.
Authors: Canal Et al.
Psychopharmacology (Berl) 2010;209:163
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Locomotion after spinal cord injury depends on constitutive activity in serotonin receptors.
Authors: Fouad Et al.
J Neurophysiol 2010;104:2975
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