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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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A N James et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 17(1), 76-82 (2005-01-27)
Selective serotonin reuptake inhibitors (SSRIs) are increasingly used to treat a variety of disorders but have gastrointestinal side-effects. To determine the effects of the SSRI, fluoxetine, on gastric smooth muscle contractility. Fundic, antral, and pyloric circular muscle contractility of guinea
Lucie Rivail et al.
British journal of pharmacology, 143(3), 361-370 (2004-09-08)
A body of evidences suggests that a hydrophobic pocket of the human 5-HT(4) receptor contributes to the high affinity of some bulky 5-HT(4) ligands. A thorough study of this pocket was performed using mutagenesis and molecular modeling. Ligand binding or
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
J Kamei et al.
Neuroscience, 174, 224-233 (2010-11-18)
Respiratory depression is the most well-known and dangerous side-effect of opioid analgesics. Clinical investigations have revealed that this opioid-induced respiratory depression is less severe in patients with chronic pain, but the mechanisms that underlie this phenomenon are unknown. Therefore, the
Tadayoshi Mikami et al.
Journal of pharmacological sciences, 107(3), 251-259 (2008-07-01)
In the present study, binding affinities of 5-hydroxytryptamine-4 (5-HT(4)) ligands for the human 5-HT(4d) receptor were determined using the agonist [(3)H]5-HT and the selective 5-HT(4) antagonist [(3)H]GR113,808. We also compared the affinity differences between [(3)H]5-HT binding (K(H)) and [(3)H]GR113,808 binding
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