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Submit ReviewSB 206553 hydrochloride
Description: Potent and selective 5-HT2B and 5-HT2C 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)
Biological Activity for SB 206553 hydrochloride
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.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries for SB 206553 hydrochloride
SB 206553 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SB 206553 hydrochloride
| 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 for SB 206553 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.88 | 100 |
Preparing Stock Solutions for SB 206553 hydrochloride
The following data is based on the product molecular weight 328.8. Batch specific molecular weights may vary from batch to batch due to the degree 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 for SB 206553 hydrochloride
References for SB 206553 hydrochloride
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 DA release induced in vivo by amphetamine and mor. 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
9 Citations for SB 206553 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 206553 hydrochloride include:
Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438
Bigford et al (2012) 5-Hydroxytryptamine 5HT2C receptors form a protein complex with N-MthD.-aspartate GluN2A subunits and activate phosphorylation of Src protein to modulate motoneuronal depolarization. J Biol Chem 287 11049 PMID: 22291020
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
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
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
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
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
Do you know of a great paper that uses SB 206553 hydrochloride from Tocris? Please let us know.
Reviews for SB 206553 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Effects of SB-206553 on MDMA-induced changes in dorsal striatal electrophysiology.
By
Kevin Ball on 01/25/2019
Assay Type: In Vivo
Species: Rat
We assessed the effect of SB-206553 (2.0 mg/kg, s.c.) on dorsal striatal single-unit electrophysiology following MDMA (ecstasy; 5.0 mg/kg) administration. A coefficient-of-variation analysis indicated significantly less variability in the magnitude of both MDMA-induced neuronal excitations and inhibitions in rats that were pretreated with SB-206553 compared to vehicle (shown in figure).
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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