SB 269970 hydrochloride

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Cat.No. 1612 - SB 269970 hydrochloride | C18H28N2O3S.HCl | CAS No. 261901-57-9
Description: Potent and selective 5-HT7 antagonist; brain penetrant
Chemical Name: (2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (12)
Literature

Biological Activity

Potent and selective 5-HT7 receptor antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B and < 6.0 for 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4 and 5-HT6 receptors respectively). Brain penetrant in vivo.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Compound Libraries

SB 269970 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 388.95
Formula C18H28N2O3S.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 261901-57-9
PubChem ID 11957684
InChI Key XQCJOYZLWFNDIO-PKLMIRHRSA-N
Smiles OC1=CC(S(N2[C@@H](CCN3CCC(C)CC3)CCC2)(=O)=O)=CC=C1.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.89 100
water 7.78 20
phosphate buffered saline 1.76 5

Preparing Stock Solutions

The following data is based on the product molecular weight 388.95. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.57 mL 12.86 mL 25.71 mL
5 mM 0.51 mL 2.57 mL 5.14 mL
10 mM 0.26 mL 1.29 mL 2.57 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Hagan et al (2000) Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist. Br.J.Pharmacol. 130 539 PMID: 10821781

Kogan et al (2002) DR4004, a putative 5-HT7 receptor antagonist, also has functional activity at the dopamine receptor. Eur.J.Pharmacol. 449 105 PMID: 12163113

Lovell et al (2000) A novel, potent, and selective 5-HT7 antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970) J.Med.Chem. 43 342 PMID: 10669560


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Keywords: Potent selective 5-HT7 antagonists Brain penetrant Serotonin Receptors 5-Hydroxytryptamine SB269970 hydrochloride GlaxoSmithKline GSK 5-HT7 Receptors

12 Citations for SB 269970 hydrochloride

Citations are publications that use Tocris products. Selected citations for SB 269970 hydrochloride include:

Speranza et al (2015) Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics. J Biomed Sci 9 62 PMID: 25814944

Watts et al (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. J Immunol 3 e00103 PMID: 25692021

Chien and Su (2015) 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts. Pharmacol Res Perspect 22 42 PMID: 26076928

Watanabe et al (2014) Effect of peripheral 5-HT on glucose and lipid metabolism in wether sheep. PLoS One 9 e88058 PMID: 24505376

Corcoran et al (2014) Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice. Front Behav Neurosci 34 51 PMID: 24381267

Kim et al (2013) Targeted inhibition of serotonin type 7 (5-HT7) receptor function modulates immune responses and reduces the severity of intestinal inflammation. J Biol Chem 190 4795 PMID: 23554310

Nikiforuk et al (2013) Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on ketamine-induced schizophrenia-like deficits in rats. PLoS One 8 e66695 PMID: 23776692

Soll et al (2012) Expression of serotonin receptors in human hepatocellular cancer. Clin Cancer Res 18 5902 PMID: 23087410

Bonaventure et al (2011) Pharmacological blockade of serotonin 5-HT7 receptor reverses working memory deficits in rats by normalizing cortical glutamate neurotransmission. PLoS One 6 e20210 PMID: 21701689

Manzke et al (2009) Serotonin targets inhibitory synapses to induce modulation of network functions. Philos Trans R Soc Lond B Biol Sci 364 2589 PMID: 19651659

Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285

Madden and Morrison (2008) Brown adipose tissue sympathetic nerve activity is potentiated by activation of 5-hydroxytryptamine (5-HT)1A/5-HT7 receptors in the rat spinal cord. Neuropharmacology 54 487 PMID: 18082230


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