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G5918

Sigma-Aldrich

GR 113808

≥98% (HPLC), solid

Sinônimo(s):

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

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About This Item

Fórmula empírica (Notação de Hill):
C19H27N3O4S
Número CAS:
144625-51-4
Peso molecular:
393.50
Número MDL:
MFCD00912901
Código UNSPSC:
12352200
ID de substância PubChem:
24278311
NACRES:
NA.77

R$ 1.745,00

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Ensaio

≥98% (HPLC)

Formulário

solid

cor

white to light pink

solubilidade

DMSO: >20 mg/mL

originador

GlaxoSmithKline

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

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

chave InChI

MOZPSIXKYJUTKI-UHFFFAOYSA-N

Informações sobre genes

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

Aplicação

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.[1] It has also been used as a 5-HT4R antagonist to study its effects on de novo enteric neurogenesis in post-embryonic zebrafish.[2]

Ações bioquímicas/fisiológicas

GR 113808 is a 5-HT4 serotonin receptor antagonist.

Características e benefícios

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

Informações legais

Sold for research purposes under agreement from Glaxo­Smith­Kline

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

Eyeshields, Gloves, type N95 (US)

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Certificados de análise (COA)

Lot/Batch Number
0000134836
0000099426
0000083061
0000083073
0000066441

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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
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
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
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