GR113808

Names

[ Name ]:
GR113808

[Synonym ]:
Clocinnamox mesylate
MFCD00912901
1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate

Biological Activity

[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/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling 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

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

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...