G5918
GR 113808
≥98% (HPLC), solid
别名:
1-[2-[（甲磺酰基）氨基]乙基]-4-哌啶基]甲基1-甲基-1H-吲哚-3-羧酸酯
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选择尺寸
关于此项目
经验公式（希尔记法）:
C19H27N3O4S
化学文摘社编号:
分子量:
393.50
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
GR 113808, ≥98% (HPLC), solid
InChI key
MOZPSIXKYJUTKI-UHFFFAOYSA-N
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
assay
≥98% (HPLC)
form
solid
color
white to light pink
solubility
DMSO: >20 mg/mL
originator
GlaxoSmithKline
storage temp.
2-8°C
Quality Level
Gene Information
human ... HTR4(3360)
rat ... Htr3a(79246), Htr4(25324)
Application
GR 113808已被用作5-羟色胺受体4（5-HT4R）阻断剂，以研究其对大鼠心室心肌细胞中钙（Ca2+）瞬变的影响。它也已被用作5-HT4R拮抗剂，以研究其对胚胎后斑马鱼从头肠神经发生的影响。
Biochem/physiol Actions
GR 113808是5-HT4血清素受体拮抗剂。
Features and Benefits
该化合物由 GlaxoSmithKline开发。想浏览其他制药公司开发的化合物和已批准药物/候选药物目录， 请单击此处。
Legal Information
根据GlaxoSmithKline的协议出售用于研究目的
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
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
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
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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