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G5918

GR 113808

Name: GR 113808
Brand: SIGMA

≥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

NACRES:

NA.77

PubChem Substance ID:

24278311

UNSPSC Code:

12352200

MDL number:

MFCD00912901

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

200

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Quality Level

200

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)

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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

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Upregulation of mucosal 5-HT3 receptors is involved in restoration of colonic transit after pelvic nerve transection.

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

Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants.

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

5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice.

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

Secondary mechanical allodynia and hyperalgesia depend on descending facilitation mediated by spinal 5-HT₄, 5-HT₆ and 5-HT₇ receptors.

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

Effect of chronic pain on morphine-induced respiratory depression in mice.

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

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Global Trade Item Number

SKU	GTIN
G5918-50MG	04061832082240
G5918-10MG	04061832091006

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