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G5918

Sigma-Aldrich

GR 113808

≥98% (HPLC), solid

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C19H27N3O4S
Numéro CAS:
144625-51-4
Poids moléculaire :
393.50
Numéro MDL:
MFCD00912901
Code UNSPSC :
12352200
ID de substance PubChem :
24278311
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

solid

Couleur

white to light pink

Solubilité

DMSO: >20 mg/mL

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne 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

Clé InChI

MOZPSIXKYJUTKI-UHFFFAOYSA-N

Informations sur le gène

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.

Actions biochimiques/physiologiques

GR 113808 is a 5-HT4 serotonin receptor antagonist.

Caractéristiques et avantages

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

Informations légales

Sold for research purposes under agreement from Glaxo­Smith­Kline

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

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
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
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
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
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
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