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GR 113808

  Cat. No.:  DC28147   Featured
Chemical Structure
144625-51-4
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More than 5000 active chemicals with high quality for research!
Field of application
GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 144625-51-4
Chemical Name: 1H-Indole-3-carboxylicacid, 1-methyl-, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
Synonyms: 1H-Indole-3-carboxylicacid, 1-methyl-, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester;[1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate;1H-Indole-3-carboxylicacid, 1-methyl-, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methy...;GR 113808;1-[2-(METHYLSULFONYL)-AMINO]ETHYL-4-PIPERIDINYLMETHYL 1-METHYL-1H-INDOLE-3-CARBOXYLATE;1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate;1-METHYL-1H-INDOLE-3-CARBOXYLIC ACID,[1-[2-[(METHYLSULFONYL)AMINO]ETHYL]-4-PIPERIDINYL]METHYL ESTER;Clocinnamox mesylate
SMILES: CS(NCCN1CCC(COC(C2=CN(C)C3=CC=CC=C23)=O)CC1)(=O)=O
Formula: C19H27N3O4S
M.Wt: 393.500383615494
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors[1].
In Vivo: GR113808 (intraperitoneal injection; 1 mg/kg; 5-7 days starting 24 h after induction of colitis) shows a significant increase in the disease activity index (DAI),which includes evaluation of weight loss, stool consistency, and presence of fecal blood[2]. Animal Model: Mice[1] Dosage: 1 mg/Kg Administration: Intraperitoneal injection; 1 mg/Kg; 5-7 days starting 24 h after induction of colitis Result: Blocked protective effects of tegaserod after induction of colitis.
References: [1]. Gale JD, et al. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.Br J Pharmacol. 1994 Jan;111(1):332-8. [2]. Spohn SN, et al.Protective Actions of Epithelial 5-Hydroxytryptamine 4 Receptors in Normal and Inflamed Colon.Gastroenterology. 2016 Nov;151(5):933-944.e3.
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