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Submit ReviewGR 113808
说明： Potent and selective 5-HT4 antagonist
化学名： 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
纯度： ≥98% (HPLC)
生物活性 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.
许可信息
Sold with the permission of GlaxoSmithKline
技术数据 for GR 113808
| 分子量 | 393.5 |
| 公式 | C19H27N3O4S |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GR 113808
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. HCl | 9.84 | 25 |
制备储备液 for GR 113808
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for GR 113808
参考文献 for GR 113808
参考文献是支持产品生物活性的出版物。
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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关键词: GR 113808, GR 113808 supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR113808, GlaxoSmithKline, GSK, 1322, Tocris Bioscience
5 篇 GR 113808 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GR 113808 的部分引用包括：
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
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
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.