SB 206553 hydrochloride

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Cat.No. 1661 - SB 206553 hydrochloride | C17H16N4O.HCl | CAS No. 1197334-04-5
Description: Potent, selective 5-HT2C/5-HT2B antagonist. Orally active
Chemical Name: 3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Reviews
Literature

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

SB 206553 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 328.8
Formula C17H16N4O.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1197334-04-5
PubChem ID 11957707
InChI Key VGEMBOFBPSNOIO-UHFFFAOYSA-N
Smiles Cl.CN1C=CC2=CC3=C(CCN3C(=O)NC3=CC=CN=C3)C=C12

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.88 100

Preparing Stock Solutions

The following data is based on the product molecular weight 328.8. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.04 mL 15.21 mL 30.41 mL
5 mM 0.61 mL 3.04 mL 6.08 mL
10 mM 0.3 mL 1.52 mL 3.04 mL
50 mM 0.06 mL 0.3 mL 0.61 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Forbes et al (1995) 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. J.Med.Chem. 38 2524 PMID: 7629791

Kennett et al (1996) In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. Br.J.Pharmacol. 117 427 PMID: 8821530

Porras et al (2002) 5-HT2A and 5-HT2C/2B receptor subtypes modulate dopamine release induced in vivo by amphetamine and morphine in both the rat nucleus accumbens and striatum. Neuropsychopharmacology 26 311 PMID: 11850146


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Keywords: SB 206553 hydrochloride, SB 206553 hydrochloride supplier, Potent, selective, 5-HT2C/5-HT2B, antagonists, Serotonin, 5-HT2B, Receptors, 5-HT2C, SB206553, hydrochloride, GlaxoSmithKline, GSK, 1661, Tocris Bioscience

8 Citations for SB 206553 hydrochloride

Citations are publications that use Tocris products. Selected citations for SB 206553 hydrochloride include:

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

Murray et al (2010) Recovery of motoneuron and locomotor function after spinal cord injury depends on constitutive activity in 5-HT2C receptors. Nat Med 16 694 PMID: 20512126

Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-methyl-D-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020

Delaney et al (2011) Pulmonary vascular effects of serotonin and selective serotonin reuptake inhibitors in the late-gestation ovine fetus. Am J Physiol Lung Cell Mol Physiol 301 L937 PMID: 21908589

Kuo et al (2014) A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases. Int J Biol Sci 10 64 PMID: 24391452

Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833

Li et al (2014) Synthesis, transport, and metabolism of serotonin formed from exogenously applied 5-HTP after spinal cord injury in rats. J Neurophysiol 111 145 PMID: 24068759


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