SB 269970 hydrochloride

Pricing Availability   Qty
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 (17)
Reviews
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 7.78 20
DMSO 38.89 100

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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:

References

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

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


If you know of a relevant reference for SB 269970 hydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all 5-HT7 Receptor Antagonists

Keywords: SB 269970 hydrochloride, SB 269970 hydrochloride supplier, Potent, selective, 5-HT7, antagonists, Brain, penetrant, Serotonin, Receptors, 5-Hydroxytryptamine, SB269970, hydrochloride, GlaxoSmithKline, GSK, 1612, Tocris Bioscience

17 Citations for SB 269970 hydrochloride

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

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

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

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

Speranza (2017) Serotonin 5-HT7 receptor increases the density of dendritic spines and facilitates synaptogenesis in forebrain neurons J Neurochem 141 647 PMID: 28122114

Bijata (2017) Synaptic Remodeling Depends on Signaling between Serotonin Receptors and the Extracellular Matrix Cell Rep 19 1767 PMID:  28564597

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

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

Gautam et al (2016) Tryptophan hydroxylase 1 and 5-HT7 receptor preferentially expressed in triple-negative breast cancer promote cancer progression through autocrine serotonin signaling. Mol Cancer 15 75 PMID: 27871326

Huang et al (2009) Repeated cocaine administration decreases 5-HT(2A) receptor-mediated serotonergic enhancement of synaptic activity in rat medial prefrontal cortex. Neuropsychopharmacology 34 1979 PMID: 19212317

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

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

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

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

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 269970 hydrochloride from Tocris? Please let us know.

Reviews for SB 269970 hydrochloride

There are currently no reviews for this product. Be the first to review SB 269970 hydrochloride and earn rewards!

Have you used SB 269970 hydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
5-HT Receptors

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.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.