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G5918

Sigma-Aldrich

GR 113808

≥98% (HPLC), solid

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C19H27N3O4S
CAS-Nummer:
144625-51-4
Molekulargewicht:
393.50
MDL-Nummer:
MFCD00912901
UNSPSC-Code:
12352200
PubChem Substanz-ID:
24278311
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

solid

Farbe

white to light pink

Löslichkeit

DMSO: >20 mg/mL

Ersteller

GlaxoSmithKline

Lagertemp.

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

InChIKey

MOZPSIXKYJUTKI-UHFFFAOYSA-N

Angaben zum Gen

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

Anwendung

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. Wirkung

GR 113808 is a 5-HT4 serotonin receptor antagonist.

Leistungsmerkmale und Vorteile

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

Rechtliche Hinweise

Sold for research purposes under agreement from Glaxo­Smith­Kline

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)

Analysenzertifikate (COA)

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Sigma-Aldrich

Sigma-Aldrich

H6648

Hanks-Salze -Lösung

Polyethylenglykol 400, for synthesis

Sigma-Aldrich

8.07485

Polyethylenglykol

Dispase® II (neutrale Protease, Klasse II) lyophilized, from bacterial, Roche, pkg of 5 × 1 g

Roche

04942078001

Dispase® II (neutrale Protease, Klasse II)

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
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
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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