Catalog Number: 1612
Chemical Name: (2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine hydrochloride
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.
Technical Data
  • M.Wt:
    388.95
  • Formula:
    C18H28N2O3S.HCl
  • Solubility:
    Soluble to 20 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    261901-57-9
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.
Background References
  1. Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist.
    Hagan et al.
    Br.J.Pharmacol., 2000;130:539
  2. DR4004, a putative 5-HT7 receptor antagonist, also has functional activity at the dopamine receptor.
    Kogan et al.
    Eur.J.Pharmacol., 2002;449:105
  3. 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
Citations:

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

14 Citations: Showing 1 - 10
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  1. Synaptic Remodeling Depends on Signaling between Serotonin Receptors and the Extracellular Matrix
    Authors: Bijata
    Cell Rep 2017;19:1767
  2. Serotonin 5-HT7 receptor increases the density of dendritic spines and facilitates synaptogenesis in forebrain neurons
    Authors: Speranza
    J Neurochem 2017;141:647
  3. 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
  4. 5-HT is a potent relaxant in rat superior mesenteric veins.
    Authors: Watts Et al.
    J Immunol 2015;3:e00103
  5. 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
  6. Effect of peripheral 5-HT on glucose and lipid metabolism in wether sheep.
    Authors: Watanabe Et al.
    PLoS One 2014;9:e88058
  7. Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice.
    Authors: Corcoran Et al.
    Front Behav Neurosci 2014;34:51
  8. Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on ketamine-induced schizophrenia-like deficits in rats.
    Authors: Nikiforuk Et al.
    PLoS One 2013;8:e66695
  9. 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
  10. Expression of serotonin receptors in human hepatocellular cancer.
    Authors: Soll Et al.
    Clin Cancer Res 2012;18:5902
  11. 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
  12. 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
  13. 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
  14. 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
Expand to show all 14 Citations

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