GR 113808
Chemical Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Central 5-HT4 receptors.
Eglen et al.
TiPS, 1995;16:391 -
GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.
Gale et al.
Br.J.Pharmacol., 1994;111:332 -
An improved in vitro bioassay for the study of 5-HT4 receptors in the human isolated large intestinal circular muscle.
Prins et al.
Br.J.Pharmacol., 2000;129:1601 -
Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Van den Wyngaert et al.
J.Neurochem., 1997;69:1810
Product Datasheets
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Citations for GR 113808
The citations listed below are publications that use Tocris products. Selected citations for GR 113808 include:
5 Citations: Showing 1 - 5
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Visceral analgesic effect of 5-HT(4) receptor agonist in rats involves the rostroventral medulla (RVM).
Authors: Sengupta Et al.
Neuropharmacology 2014;79:345
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Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons.
Authors: Mondal Et al.
PLoS One 2013;8:e60365
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The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties.
Authors: Beattie Et al.
Front Pharmacol 2011;2:25
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Raphé neurons stimulate respiratory circuit activity by multiple mechanisms via endogenously released serotonin and substance P.
Authors: Ptak Et al.
PLoS One 2009;29:3720
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Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Diabetologia 2007;50:1743
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