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形狀
solid
顏色
off-white
溶解度
ethanol: 4.0 mg/mL
DMSO: >50 mg/mL
H2O: 8.5 mg/mL
SMILES 字串
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 密鑰
ABTNETSDXZBJTE-WLHGVMLRSA-N
基因資訊
human ... OPRK1(4986)
應用
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.
法律資訊
Sold for research purposes under agreement from GlaxoSmithKline
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
British journal of pharmacology, 110(1), 303-309 (1993-09-01)
1. The evidence for kappa-receptor heterogeneity is equivocal. We have now investigated this question by comparing the effects of five putatively selective kappa-agonists. The parameters examined were: the relative potencies in depressing hindlimb flexor muscle reflexes to noxious pinch stimuli
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
Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova, 92(12), 1419-1428 (2007-05-26)
It was found that pretreatment of rats with selective agonist of kappa1-opioid receptors (OR) (-)--U--50.488 decreased the incidence of ischemic (10 min) and reperfusion (10 min) ventricular arrhythmias. The selective kappa2-OR agonist GR-89696 had no effect on the incidence of
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 46(3), 484-494 (2005-03-08)
Brain kappa-opioid receptors (ORs) may be involved in several pathologic conditions, such as addiction, psychosis, and seizures. (+/-)-4-Methoxycarbonyl-2-[(1-pyrrolidinylmethyl]-1-[(3,4-dichlorophenyl)acetyl]-piperidine (GR89696) is a potent and selective kappa-OR agonist. The (-)-isomer, GR103545, is the active enantiomer of GR89696. The aim of this study
Bulletin of experimental biology and medicine, 145(6), 696-699 (2008-12-27)
Chronic treatment with opioid receptor ligands: nonselective peptide opioid receptor agonist dalargin (intraperitoneally in a dose of 1 mg/kg), selective nonpeptide kappa-receptor agonist GR 89696 (subcutaneously in a dose of 0.03 mg/kg), nonselectrive nonpeptide antagonist quadazocine (subcutaneously in a dose
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