CAS 144625-51-4|GR113808
| Common Name | GR113808 | ||
|---|---|---|---|
| CAS Number | 144625-51-4 | Molecular Weight | 393.50000 |
| Density | 1.3g/cm3 | Boiling Point | 572.3ºC at 760 mmHg |
| Molecular Formula | C19H27N3O4S | Melting Point | / |
| MSDS | USA | Flash Point | 299.9ºC |
Names
| Name | [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate |
|---|---|
| Synonym | More Synonyms |
GR113808 BiologicalActivity
| 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]. |
|---|---|
| Related Catalog | Research Areas >>Inflammation/ImmunologyResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
| 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. |
Chemical & Physical Properties
| Density | 1.3g/cm3 |
|---|---|
| Boiling Point | 572.3ºC at 760 mmHg |
| Molecular Formula | C19H27N3O4S |
| Molecular Weight | 393.50000 |
| Flash Point | 299.9ºC |
| Exact Mass | 393.17200 |
| PSA | 89.02000 |
| LogP | 3.00590 |
| Vapour Pressure | 4.19E-13mmHg at 25°C |
| Index of Refraction | 1.613 |
| InChIKey | MOZPSIXKYJUTKI-UHFFFAOYSA-N |
| SMILES | Cn1cc(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)c2ccccc21 |
| Storage condition | 2-8°C |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
Articles25
More Articles| Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines. Bioorg. Med. Chem. 17 , 2607-2622, (2009) Based on the definition of a 5-HT(4) receptor antagonist pharmacophore, a series of pyrrolo[1,2-a]thieno[3,2-e] and pyrrolo[1,2-a]thieno[2,3-e] pyrazine derivatives were designed, prepared, and evalua... | |
| Dual role of serotonin in the pathogenesis of indomethacin-induced small intestinal ulceration: pro-ulcerogenic action via 5-HT3 receptors and anti-ulcerogenic action via 5-HT4 receptors. Pharmacol. Res. 66(3) , 226-34, (2012) Serotonin (5-HT) exerts multiple physiological functions not only in the central and peripheral nervous systems but also in the gastrointestinal tract, and these multiple functions are accounted for b... | |
| Molecular characterization of a purified 5-HT4 receptor: a structural basis for drug efficacy. J. Biol. Chem. 280(21) , 20253-60, (2005) Serotonin 5-HT(4(a)) receptor, a G-protein-coupled receptor (GPCR), was produced as a functional isolated protein using Escherichia coli as an expression system. The isolated receptor was characterize... |
Synonyms
| Clocinnamox mesylate |
| MFCD00912901 |
| 1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate |
