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Merck
CN

I122

ICI 204,448 hydrochloride

solid

Synonym(s):

(±)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride, R,S-[3-[1-[[(3,4-Dichlorophenyl)acetyl]methylamino]-2-(1-pyrrolidinyl)ethyl] phenoxy]-acetic acid hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C23H26Cl2N2O4 · HCl
CAS Number:
121264-04-8
Molecular Weight:
501.83
NACRES:
NA.77
PubChem Substance ID:
24278040
UNSPSC Code:
12352200
MDL number:
MFCD00153814
Form:
solid

Key Documents

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form

solid

color

white

solubility

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 12 mg/mL, dilute sodium carbonate: 4 mg/mL, H2O: 4.5 mg/mL

SMILES string

Cl[H].CN(C(CN1CCCC1)c2cccc(OCC(O)=O)c2)C(=O)Cc3ccc(Cl)c(Cl)c3

InChI

1S/C23H26Cl2N2O4.ClH/c1-26(22(28)12-16-7-8-19(24)20(25)11-16)21(14-27-9-2-3-10-27)17-5-4-6-18(13-17)31-15-23(29)30;/h4-8,11,13,21H,2-3,9-10,12,14-15H2,1H3,(H,29,30);1H

InChI key

FNDGLVOYAQNQPE-UHFFFAOYSA-N

Gene Information

human ... OPRK1(4986)

Biochem/physiol Actions

κ opioid receptor agonist that does not cross the blood-brain barrier.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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M McIntosh et al.
European journal of pharmacology, 210(1), 37-44 (1992-01-07)
The antiarrhythmic activities of 16-methylcyprenorphine (M8008), nor-binaltorphimine (NBT) and naltrexone, which are relatively specific opioid receptor antagonists for delta, kappa and mu receptors, respectively, were examined during the 30 min following coronary artery occlusion in anaesthetised rats. The haemodynamic and
E R Butelman et al.
Psychopharmacology, 147(1), 73-80 (1999-12-11)
The dynorphins are endogenous opioid peptides with relative binding selectivity for kappa-receptors. It is unclear whether the dynorphins share the pharmacological profile observed with synthetic kappa-agonists in primates. The main objective of this study was to compare the effects of
A Barber et al.
British journal of pharmacology, 113(4), 1317-1327 (1994-12-01)
1. The pharmacological properties of the novel diarylacetamide kappa-opioid receptor agonist, EMD 61753, have been compared with those of ICI 197067 (a centrally-acting kappa agonist) and ICI 204448 (a peripherally-selective kappa agonist). 2. EMD 61753 binds with high affinity (IC50
R A Hirst et al.
Neuroscience letters, 232(2), 119-122 (1997-08-29)
This study describes the coupling of the recombinant rat kappa-opioid receptor expressed in Chinese hamster ovary (CHO) cells to adenylyl cyclase and the effects of receptor density. The binding of [3H]diprenorphine ([3H]DPN) was dose dependent and saturable in membranes prepared
Scott M Rawls et al.
Pharmacology, 74(2), 79-83 (2005-02-03)
ICI 204448, a selective kappa-opioid agonist with limited CNS access, can be used to discriminate central and peripheral opioid actions on physiological systems such as pain and thermoregulation. Therefore, we investigated the effect of ICI 204448 (2.5, 5, and 10
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Global Trade Item Number

SKUGTIN
I122-25MG04061832556789
I122-5MG04061832556796

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