GR 113808

Name: GR 113808
Brand: Tocris Bioscience
SKU: 1322

Catalog # 1322 | Tocris Bioscience a Bio-Techne Brand

Citations (5)

COA / SDS

Potent and selective 5-HT4 antagonist

Key Product Details

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)
Molecular Weight:	393.5

View Full Technical Details for GR 113808

Technical Data
Citations (5) / Reviews

Biological Activity for GR 113808

GR 113808 is a potent, selective 5-HT₄ receptor antagonist (pK_B = 9.43 in human colonic muscle, and K_d = 0.15 nM for binding to cloned human 5-HT₄ receptors). Displays > 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C 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 for GR 113808

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	0.20 mL	1.02 mL	2.03 mL

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References for GR 113808

References are publications that support the biological activity of the product.

Prins An improved in vitro bioassay for the study of 5-HT₄ receptors in the human isolated large intestinal circular muscle. Br.J.Pharmacol. 2000 PMID: 10780964
Van den Wyngaert Cloning and expression of a human serotonin 5-HT₄ receptor cDNA. J.Neurochem. 1997 PMID: 9349523
Eglen Central 5-HT₄ receptors. TiPS 1995 PMID: 8578609
Gale GR113808: a novel, selective antagonist with high affinity at the 5-HT₄ receptor. Br.J.Pharmacol. 1994 PMID: 8012715

Citations for GR 113808 (5)

Showing 1 - 5 of 5 citations Showing All

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Citations are publications that use Bio-Techne 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

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