G133
GR 89696 fumarate salt
solid
别名:
4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid methyl ester fumarate salt
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关于此项目
经验公式（希尔记法）:
C19H25Cl2N3O3 · C4H4O4
化学文摘社编号:
分子量:
530.40
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
表单
solid
质量水平
颜色
off-white
溶解性
ethanol: 4.0 mg/mL
DMSO: >50 mg/mL
H2O: 8.5 mg/mL
SMILES字符串
OC(=O)\C=C\C(O)=O.COC(=O)N1CCN(C(CN2CCCC2)C1)C(=O)Cc3ccc(Cl)c(Cl)c3
InChI
1S/C19H25Cl2N3O3.C4H4O4/c1-27-19(26)23-8-9-24(15(13-23)12-22-6-2-3-7-22)18(25)11-14-4-5-16(20)17(21)10-14;5-3(6)1-2-4(7)8/h4-5,10,15H,2-3,6-9,11-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
InChI key
ABTNETSDXZBJTE-WLHGVMLRSA-N
基因信息
human ... OPRK1(4986)
相关类别
应用
GR 89696 fumarate salt has been used as a κ κ2 opioid receptor (KOR) agonist to study its anti-scratching and antipruritic effects on monkeys.
生化/生理作用
GR 89696 fumarate is a selective κ2 opioid receptor agonist.
法律信息
Sold for research purposes under agreement from GlaxoSmithKline
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)
R M Caudle et al.
The Journal of pharmacology and experimental therapeutics, 283(3), 1342-1349 (1998-02-12)
Receptor binding studies and electrophysiological studies demonstrated the existence of at least two kappa opioid receptors, which have been designated kappa-1 and kappa-2. Several agonists and antagonists are selective for the kappa-1 receptor whereas no known ligands are selective for
A Naylor et al.
Journal of medicinal chemistry, 36(15), 2075-2083 (1993-07-23)
The synthesis of 4-substituted 1-(arylacetyl)-2-[(alkylamino)methyl]piperazines (10-22, 26, 27, and 30-33) and their activities as kappa-opioid receptor agonists are described. This includes a range of 4-acyl and 4-carboalkoxy derivatives with the latter series showing the greatest kappa-agonist activity. In particular, methyl
Giampaolo Tomasi et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 54(4), 600-608 (2013-02-21)
The κ-opioid receptors (KOR) are involved in mood disorders and addictive conditions. In vivo imaging studies of this receptor in humans have not been reported because of the lack of a selective ligand. We used a recently developed selective KOR
Stephanie N Washburn et al.
Neurobiology of learning and memory, 89(1), 1-16 (2007-11-07)
Spinal cord neurons can support a simple form of instrumental learning. In this paradigm, rats completely transected at the second thoracic vertebra learn to minimize shock exposure by maintaining a hindlimb in a flexed position. Prior exposure to uncontrollable shock
Mei-Chuan Ko et al.
The Journal of pharmacology and experimental therapeutics, 328(1), 193-200 (2008-10-10)
Itch/pruritus is the most common side effect associated with spinal administration of morphine given to humans for analgesia. The aim of this study was to investigate the effectiveness of kappa-opioid receptor (KOR) agonists with diverse chemical structures as antipruritics and
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