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Documenti fondamentali

I122

Sigma-Aldrich

ICI 204,448 hydrochloride

solid

Sinonimo/i:

(±)-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

Formula empirica (notazione di Hill):
C23H26Cl2N2O4 · HCl
Numero CAS:
Peso molecolare:
501.83
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

Stato

solid

Colore

white

Solubilità

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

Stringa SMILE

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
FNDGLVOYAQNQPE-UHFFFAOYSA-N

Informazioni sul gene

human ... OPRK1(4986)

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Azioni biochim/fisiol

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

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)


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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
H Keïta et al.
European journal of pharmacology, 277(2-3), 275-280 (1995-04-24)
The antinociceptive effect of intraplantar (i.pl.) ICI 204448 ((R,S)-N-[2-(N-methyl-3,4-dichloro-phenylacetamido)-2-(3-carbox yph enyl)- ethyl]pyrrolidine hydrochloride)) (20, 30, 40 and 50 micrograms), a kappa-opioid receptor agonist which has limited access to the central nervous system, was studied in a well-established rat model of
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
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
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

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