ICI 204,448 hydrochloride - CAS 121264-04-8
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Opioid Receptor
ICI 204,448 hydrochloride is the hydrochloride salt of ICI 204,448, which is a peripherally acting κ opioid receptor agonist. It does not cross the blood-brain barrier.
≥98% by HPLC
ICI 204,448 hydrochloride; ICI204,448 hydrochloride; ICI-204,448 hydrochloride; (±)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride; (RS)-[3-[1-[[(3,4-Dichlorophenyl)acetyl]methylamino]-2-(1-pyrrolidinyl)ethyl]phenoxy]acetic acid hydrochloride
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1.Elevation of atrial natriuretic peptide levels in aqueous humor of the rabbit by kappa opioid receptor agonists.
Russell KR;Moore TT;Potter DE Neuropeptides. 2001 Oct-Dec;35(5-6):232-7.
Following the topical administration of three kappa agonists (bremazocine, spiradoline and ICI 204448) to rabbit eyes, aqueous humor samples were analyzed for levels of atrial natriuretic peptide (ANP). Bremazocine (BRE) and spiradoline (SPR) elevated aqueous ANP levels in a dose-dependent manner. In contrast, ICI had no significant effect on ANP levels in aqueous humor. Nor-binaltorphimine (nor-BNI), a selective kappa opioid receptor antagonist, was used to assess kappa opioid receptor involvement and glibenclamide, an ATP-sensitive K+ channel blocker, was used to test for the role of ATP-sensitive potassium channels in ANP release. Pretreatment with nor-BNI antagonized the increases in ANP levels observed with both BRE and SPR. Likewise, glibenclamide suppressed the stimulation of ANP secretion by bremazocine. In summary, BRE and SPR increased ANP levels in aqueous humor of rabbits, in part, via activation of K+(ATP) channels that are assumed to be associated with kappa opioid receptors.
2.Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists.
Carey GJ;Bergman J J Pharmacol Exp Ther. 2001 Apr;297(1):215-23.
Squirrel monkeys were trained to discriminate i.m. injections of the kappa-opioid receptor agonist enadoline (0.0017 mg/kg) from saline in a two-lever drug-discrimination procedure. Enadoline produced a reliable discriminative stimulus that was reproduced by the kappa-selective agonists PD 117302, U 50,488, GR 89686A, (-)-spiradoline, ICI 204448, and EMD 61753, and by the mixed-action kappa/mu-agonists bremazocine and ethylketocyclazocine. The discriminative stimulus effects of enadoline were not reproduced by the mu-selective agonist morphine, the delta-selective agonist BW373U86, the mixed-action opioids nalbuphine and nalorphine, or by the less active enantiomers of enadoline and spiradoline PD 129829 and (+)-spiradoline, respectively. The selective mu-opioid antagonist beta-funaltrexamine (10.0 mg/kg) did not appreciably alter the dose-effect function for enadoline in any subject. However, the nonselective and kappa-selective opioid antagonists quadazocine (0.03-3.0 mg/kg) and nor-BNI (3-10 mg/kg), and the mixed-action opioid nalbuphine (0.3-30 mg/kg) served to surmountably antagonize enadoline's discriminative stimulus effects. The antagonist effects of nor-BNI were long-lasting and did not distinguish between drugs purported to act at different kappa-receptor subtypes.
3.Peripheral kappa-opioid agonist, ICI 204448, evokes hypothermia in cold-exposed rats.
Rawls SM;Ding Z;Gray AM;Cowan A Pharmacology. 2005 May;74(2):79-83. Epub 2005 Jan 12.
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 mg/kg, s.c.) on male Sprague-Dawley rats exposed to ambient temperatures of 5, 20, or 32 degrees C. ICI 204448 did not alter the body temperature of rats maintained at 20 or 32 degrees C. However, 5 and 10 mg/kg of ICI 204448 evoked significant hypothermia in rats exposed to 5 degrees C. The i.c.v. administration of nor-BNI, a kappa-opioid antagonist, did not affect the hypothermia produced by the systemic injection of ICI 204448. Thus, an involvement of brain kappa-opioid receptors in ICI 204448-evoked hypothermia is unlikely. The present data demonstrate for the first time that ICI 204448 produces hypothermia in cold-exposed rats and suggest that the role of peripheral kappa-opioid receptors in thermoregulation becomes more significant at cold ambient temperatures.
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CAS 121264-04-8 ICI 204,448 hydrochloride

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