SB 206553 hydrochloride

Cat. No. 1661

SB 206553 hydrochloride C17H16N4O.HCl [1197334-04-5]

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Chemical Name: 3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']dipyrrole-1(2H)-carboxamide hydrochloride

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

Technical Data

Soluble to 100 mM in DMSO
>99 %
Desiccate at RT

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 / Safety Data Sheet

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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.

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.

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.

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

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.

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.

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.

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

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