GR 113808

Pricing Availability   Qty
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)
Citations (5)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

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

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.

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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

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

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.