SB 269970 hydrochloride

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SB 269970 hydrochloride | CAS No. 261901-57-9 | 5-HT7 Receptor Antagonists
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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%

Product Details
Citations (21)
Supplemental Products

Biological Activity

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.

Technical Data

Soluble to 20 mM in water and to 100 mM in DMSO
Store at +4°C

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.

Background References

  1. Targeted inhibition of serotonin type 7 (5-HT7) receptor function modulates immune responses and reduces the severity of intestinal inflammation.
    Kim, Janice J, Bridle, Byram W, Ghia, Jean-Eri, Wang, Huaqing, Syed, Shahzad, Manocha, Marcus M, Rengasamy, Palanive, Shajib, Mohammad, Wan, Yonghong, Hedlund, Peter B, Khan, Waliul I
    J Immunol, 2013;190(9):4795-804.
  2. Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist.
    Hagan et al.
    Br.J.Pharmacol., 2000;130:539
  3. DR4004, a putative 5-HT7 receptor antagonist, also has functional activity at the DA receptor.
    Kogan et al.
    Eur.J.Pharmacol., 2002;449:105
  4. A novel, potent, and selective 5-HT7 antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970)
    Lovell et al.
    J.Med.Chem., 2000;43:342

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Citations for SB 269970 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for SB 269970 hydrochloride include:

21 Citations: Showing 1 - 10

  1. 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
    Authors: Tang Et al.
    FASEB J37  2023;e22893
  2. Modulation of Gut Microbiota Composition by Serotonin Signaling Influences Intestinal Immune Response and Susceptibility to Colitis.
    Authors: Kwon Et al.
    Cell Mol Gastroenterol Hepatol  2019;7:709
  3. Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice.
    Authors: Nguyen Et al.
    Korean J Physiol Pharmacol  2019;23:271
  4. Selective Modulation of Axonal Sodium Channel Subtypes by 5-HT1A Receptor in Cortical Pyramidal Neuron.
    Authors: Yin Et al.
    Cereb Cortex  2017;27:509
  5. Synaptic Remodeling Depends on Signaling between Serotonin Receptors and the Extracellular Matrix
    Authors: Bijata
    Cell Rep  2017;19:1767
  6. Serotonin 5-HT7 receptor increases the density of dendritic spines and facilitates synaptogenesis in forebrain neurons
    Authors: Speranza
    J Neurochem  2017;141:647
  7. Tryptophan hydroxylase 1 and 5-HT7 receptor preferentially expressed in triple-negative breast cancer promote cancer progression through autocrine serotonin signaling.
    Authors: Gautam Et al.
    Mol Cancer  2016;15:75
  8. Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics.
    Authors: Speranza Et al.
    J Biomed Sci  2015;9:62
  9. 5-HT is a potent relaxant in rat superior mesenteric veins.
    Authors: Watts Et al.
    J Immunol  2015;3:e00103
  10. 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts.
    Authors: Chien and Su
    Pharmacol Res Perspect  2015;22:42
  11. Effect of peripheral 5-HT on glucose and lipid metabolism in wether sheep.
    Authors: Watanabe Et al.
    PLoS One  2014;9:e88058
  12. Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice.
    Authors: Corcoran Et al.
    Front Behav Neurosci  2014;34:51
  13. Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on KA-induced schizophrenia-like deficits in rats.
    Authors: Nikiforuk Et al.
    PLoS One  2013;8:e66695
  14. Targeted inhibition of serotonin type 7 (5-HT7) receptor function modulates immune responses and reduces the severity of intestinal inflammation.
    Authors: Kim Et al.
    J Biol Chem  2013;190:4795
  15. Expression of serotonin receptors in human hepatocellular cancer.
    Authors: Soll Et al.
    Clin Cancer Res  2012;18:5902
  16. Pharmacological blockade of serotonin 5-HT7 receptor reverses working memory deficits in rats by normalizing cortical glutamate neurotransmission.
    Authors: Bonaventure Et al.
    PLoS One  2011;6:e20210
  17. 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo.
    Authors: M&#252;ller Et al.
    PLoS One  2009;4:e6453
  18. Serotonin targets inhibitory synapses to induce modulation of network functions.
    Authors: Manzke Et al.
    Philos Trans R Soc Lond B Biol Sci  2009;364:2589
  19. Repeated cocaine administration decreases 5-HT(2A) receptor-mediated serotonergic enhancement of synaptic activity in rat medial prefrontal cortex.
    Authors: Huang Et al.
    Neuropsychopharmacology  2009;34:1979
  20. Brown adipose tissue sympathetic nerve activity is potentiated by activation of 5-hydroxytryptamine (5-HT)1A/5-HT7 receptors in the rat spinal cord.
    Authors: Madden and Morrison
    Neuropharmacology  2008;54:487
  21. Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
    Authors: Hampson Et al.
    Diabetologia  2007;50:1743


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