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SB 269970 hydrochloride
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.
Sold for research purposes under agreement from GlaxoSmithKline.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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|
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
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18 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
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
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
Watanabe et al (2014) Effect of peripheral 5-HT on glucose and lipid metabolism in wether sheep. PLoS One 9 e88058 PMID: 24505376
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
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
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
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
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
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
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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.
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.
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.