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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)
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)
Bent W Schoultz et al.
European journal of nuclear medicine and molecular imaging, 37(6), 1174-1180 (2010-02-17)
The recent development in radiosynthesis of the (11)C-carbamate function increases the potential of [(11)C]GR103545, which for the last decade has been regarded as promising for imaging the kappa-opioid receptor (kappa-OR) with PET. In the present study, [(11)C]GR103545 was evaluated in
P J Birch et al.
British journal of pharmacology, 103(3), 1819-1823 (1991-07-01)
1. The effect of a novel, highly potent and selective kappa-opioid receptor agonist, GR89696, has been evaluated in two animal models of cerebral ischaemia: transient bilateral carotid artery occlusion in the Mongolian gerbil and permanent, unilateral middle cerebral artery occlusion
J Ho et al.
The Journal of pharmacology and experimental therapeutics, 281(1), 136-141 (1997-04-01)
It has been demonstrated that kappa-2 opioid receptor agonists can inhibit the current that flows through the N-methyl-o-aspartate (NMDA) subclass of excitatory amino acid receptor. NMDA receptor antagonists have been shown to be effective antihyperalgesic agents when administered intrathecally into
Baojun Gu et al.
The Journal of urology, 171(1), 472-477 (2003-12-11)
The nonselective kappa opioid receptor agonist ethylketocyclazocine suppresses external urethral sphincter (EUS) reflexes in cats. We examined the role of spinal kappa-opioid receptor subtypes in the control of EUS function in rats using selective kappa-1 (U-50,488) or kappa-2 (GR-89,696) opiate
Woong Mo Kim et al.
Anesthesia and analgesia, 113(4), 934-940 (2011-07-27)
Although bone cancer-related pain is one of the most disruptive symptoms in patients with advanced cancer, patients are often refractory to pharmacological treatments; thus, more effective treatments for bone cancer pain are needed. We evaluated the analgesic efficacy of and
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