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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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
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
solid
颜色
white to light pink
溶解性
DMSO: >20 mg/mL
创始人
GlaxoSmithKline
储存温度
2-8°C
SMILES字符串
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
基因信息
human ... HTR4(3360)
rat ... Htr3a(79246), Htr4(25324)
应用
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。
生化/生理作用
GR 113808是5-HT4血清素受体拮抗剂。
特点和优势
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。
法律信息
根据GlaxoSmithKline的协议出售用于研究目的
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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
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
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