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144625-51-4

144625-51-4 structure
144625-51-4 structure
  • Name: GR113808
  • Chemical Name: [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate
  • CAS Number: 144625-51-4
  • Molecular Formula: C19H27N3O4S
  • Molecular Weight: 393.50000
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2018-12-22 14:06:41
  • Modify Date: 2024-01-16 18:47:01
  • 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].

Name [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate
Synonyms Clocinnamox mesylate
MFCD00912901
1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate
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
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.

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
Storage condition 2-8°C
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport