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Description: Potent and selective 5-HT4 antagonist
Chemical Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
Purity: ≥98% (HPLC)
Biological Activity for GR 113808
GR 113808 is a potent, selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, and Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). Displays > 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data for GR 113808
| M. Wt | 393.5 |
| Formula | C19H27N3O4S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 144625-51-4 |
| PubChem ID | 119376 |
| InChI Key | MOZPSIXKYJUTKI-UHFFFAOYSA-N |
| Smiles | CN1C=C(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)C2=CC=CC=C12 |
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 GR 113808
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 9.84 | 25 |
Preparing Stock Solutions for GR 113808
The following data is based on the product molecular weight 393.5. 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 |
|---|---|---|---|
| 0.25 mM | 10.17 mL | 50.83 mL | 101.65 mL |
| 1.25 mM | 2.03 mL | 10.17 mL | 20.33 mL |
| 2.5 mM | 1.02 mL | 5.08 mL | 10.17 mL |
| 12.5 mM | 0.2 mL | 1.02 mL | 2.03 mL |
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Product Datasheets for GR 113808
References for GR 113808
References are publications that support the biological activity of the product.
Eglen et al (1995) Central 5-HT4 receptors. TiPS 16 391 PMID: 8578609
Gale et al (1994) GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. Br.J.Pharmacol. 111 332 PMID: 8012715
Prins et al (2000) An improved in vitro bioassay for the study of 5-HT4 receptors in the human isolated large intestinal circular muscle. Br.J.Pharmacol. 129 1601 PMID: 10780964
Van den Wyngaert et al (1997) Cloning and expression of a human serotonin 5-HT4 receptor cDNA. J.Neurochem. 69 1810 PMID: 9349523
If you know of a relevant reference for GR 113808, please let us know.
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Keywords: GR 113808, GR 113808 supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR113808, GlaxoSmithKline, GSK, 1322, Tocris Bioscience
5 Citations for GR 113808
Citations are publications that use Tocris products. Selected citations for GR 113808 include:
Sengupta et al (2014) Visceral analgesic effect of 5-HT(4) receptor agonist in rats involves the rostroventral medulla (RVM). Neuropharmacology 79 345 PMID: 24334068
Mondal et al (2013) Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons. PLoS One 8 e60365 PMID: 23565235
Beattie et al (2011) The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol 2 25 PMID: 21687517
Ptak et al (2009) Raphé neurons stimulate respiratory circuit activity by multiple mechanisms via endogenously released serotonin and substance P. PLoS One 29 3720 PMID: 19321769
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 GR 113808 from Tocris? Please let us know.
Reviews for GR 113808
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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* 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.