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G5918

Sigma-Aldrich

GR 113808

≥98% (HPLC), solid

Synonym(s):

1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate

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About This Item

Empirical Formula (Hill Notation):
C19H27N3O4S
CAS Number:
144625-51-4
Molecular Weight:
393.50
MDL number:
MFCD00912901
UNSPSC Code:
12352200
PubChem Substance ID:
24278311
NACRES:
NA.77

Assay

≥98% (HPLC)

form

solid

color

white to light pink

solubility

DMSO: >20 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

Cn1cc(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)c3ccccc13

InChI

1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3

InChI key

MOZPSIXKYJUTKI-UHFFFAOYSA-N

Gene Information

human ... HTR4(3360)
rat ... Htr3a(79246) , Htr4(25324)

Application

GR 113808 has been used as a serotonin receptor 4 (5-HT4R) blocker to study its effects on the calcium (Ca2+) transients in rat ventricular cardiomyocytes. It has also been used as a 5-HT4R antagonist to study its effects on de novo enteric neurogenesis in post-embryonic zebrafish.

Biochem/physiol Actions

GR 113808 is a 5-HT4 serotonin receptor antagonist.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Glaxo­Smith­Kline

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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I Gribovskaja-Rupp et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 24(5), 472-478 (2012-02-07)
Colonic dysfunction occurs after pelvic autonomic nerve damage. The enteric nervous system can compensate. We investigated the role of mucosal serotonin receptors, 5-HT(3) and 5-HT(4) , in the colonic motility restoration over 2 weeks after parasympathetic pelvic nerve transection in
Kurt A Krobert et al.
Naunyn-Schmiedeberg's archives of pharmacology, 371(6), 473-479 (2005-07-14)
Prucalopride is a gastrointestinal prokinetic drug that acts through 5-HT4 receptors, but its potential effects on cardiac atrial function are unknown. We investigated the effects of prucalopride on human right atrium, piglet left atrium, and piglet sinoatrial node. The effects
M Cachard-Chastel et al.
British journal of pharmacology, 150(7), 883-892 (2007-02-28)
A strategy to treat Alzheimer's disease (AD) is to increase the soluble form of amyloid precursor protein (sAPPalpha), a promnesic protein, in the brain. Because strong evidence supports beneficial effects of 5-hydroxytryptamine 5-HT(4) receptor agonists in memory and learning, we
Guillaume Lucas et al.
Biological psychiatry, 57(8), 918-925 (2005-04-12)
We recently identified a facilitory control exerted by serotonin4 (5-HT4) receptors on the in vivo firing activity of dorsal raphe nucleus (DRN) serotonergic (5-HT) neurons. However, these findings were based on acute administrations of 5-HT4 receptor agonists and antagonists, which
B Godínez-Chaparro et al.
Neuroscience, 222, 379-391 (2012-07-17)
In the present study we determined the role of spinal 5-hydroxytriptamine (5-HT) and 5-HT(4/6/7) receptors in the long-term secondary mechanical allodynia and hyperalgesia induced by formalin in the rat. Formalin produced acute nociceptive behaviors (flinching and licking/lifting) followed by long-term
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