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Submit ReviewSB 269970 hydrochloride
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)
Biological Activity for SB 269970 hydrochloride
SB 269970 hydrochloride is a 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 for SB 269970 hydrochloride
SB 269970 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 269970 hydrochloride
| 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 for SB 269970 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 7.78 | 20 | |
| DMSO | 38.89 | 100 |
Preparing Stock Solutions for SB 269970 hydrochloride
The following data is based on the product molecular weight 388.95. 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 | 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 for SB 269970 hydrochloride
References for SB 269970 hydrochloride
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 DA 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.
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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
21 Citations for SB 269970 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 269970 hydrochloride include:
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
Kwon et al (2019) Modulation of Gut Microbiota Composition by Serotonin Signaling Influences Intestinal Immune Response and Susceptibility to Colitis. Cell Mol Gastroenterol Hepatol 7 709 PMID: 30716420
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
Yin et al (2017) Selective Modulation of Axonal Sodium Channel Subtypes by 5-HT1A Receptor in Cortical Pyramidal Neuron. Cereb Cortex 27 509 PMID: 26494800
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
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
Nguyen et al (2019) Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice. Korean J Physiol Pharmacol 23 271 PMID: 31297011
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
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
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
Nikiforuk et al (2013) Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on KA-induced schizophrenia-like deficits in rats. PLoS One 8 e66695 PMID: 23776692
Tang et al (2023) Serotonin/5-HT7 receptor provides an adaptive signal to enhance pigmentation response to environmental stressors through cAMP-PKA-MAPK, Rab27a/RhoA, and PI3K/AKT signaling pathways FASEB J37 e22893 PMID: 36961387
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
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
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5-HT has a potential for relaxant.
By
Anonymous on 02/18/2020
Assay Type: In Vivo
Species: Rat
1nM (As 5-HT7 receptor antagonists) SB 269970
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.
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.