Cat. No. 1322
Chemical Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]
Biological ActivityPotent, 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 InformationSold with the permission of GlaxoSmithKline
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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.
If you know of a relevant reference for GR 113808 please let us know.
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.
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.
Do you know of a great paper that uses GR 113808 from Tocris? If so please let us know.
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Keywords: GR 113808, supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR113808, GlaxoSmithKline, GSK, Tocris Bioscience, 5-HT4 Receptor Antagonist products
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