G5918
GR 113808
≥98% (HPLC), solid
別名:
1-[2-[(メチルスルホニル)-アミノ] エチル]-4-ピペリジニル]メチル 1-メチル-1H-インドール-3-カルボキシレート
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この商品について
実験式（ヒル表記法）:
C19H27N3O4S
CAS番号:
分子量:
393.50
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
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は、5-HT4セロトニンレセプターアンタゴニストです。
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
GlaxoSmithKlineの同意のもと、研究目的で販売しています。
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
G5918-50MG: + G5918-10MG: + G5918-VAR: + G5918-BULK:
jan
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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