SB 206553 hydrochloride
Chemical Name: 3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride
Purity: ≥99%
Biological Activity
SB 206553 hydrochloride is a potent and selective 5-HT2B/5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92). Displays > 80-fold selectivity over all other 5-HT receptor subtypes and a variety of other receptors (pKi < 6). Centrally active following oral administration in vivo.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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5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity and oral activity.
Forbes et al.
J.Med.Chem., 1995;38:2524 -
In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.
Kennett et al.
Br.J.Pharmacol., 1996;117:427 -
5-HT2A and 5-HT2C/2B receptor subtypes modulate DA release induced in vivo by amphetamine and mor. in both the rat nucleus accumbens and striatum.
Porras et al.
Neuropsychopharmacology, 2002;26:311
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Citations for SB 206553 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for SB 206553 hydrochloride include:
9 Citations: Showing 1 - 9
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Pericytes impair capillary blood flow and motor function after chronic spinal cord injury.
Authors: Li Et al.
Nat Med 2017;23:733
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Synthesis, transport, and metabolism of serotonin formed from exogenously applied 5-HTP after spinal cord injury in rats.
Authors: Li Et al.
J Neurophysiol 2014;111:145
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A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases.
Authors: Kuo Et al.
Int J Biol Sci 2014;10:64
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5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization.
Authors: Bigford Et al.
J Biol Chem 2012;287:11049
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Pulmonary vascular effects of serotonin and selective serotonin reuptake inhibitors in the late-gestation ovine fetus.
Authors: Delaney Et al.
Am J Physiol Lung Cell Mol Physiol 2011;301:L937
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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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Recovery of motoneuron and locomotor function after spinal cord injury depends on constitutive activity in 5-HT2C receptors.
Authors: Murray Et al.
Nat Med 2010;16:694
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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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Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Diabetologia 2007;50:1743
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