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Merck

G133

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C19H25Cl2N3O3 · C4H4O4
分子量:
530.40
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

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)


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J F Herrero et al.
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
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
A Iu Lishmanov et al.
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
Peter S Talbot et al.
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
Yu B Lishmanov et al.
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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