ICI 204,448 盐酸盐
ICI 204,448 盐酸盐结构式
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常用名 | ICI 204,448 盐酸盐 | 英文名 | ICI 204,448 hydrochloride |
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| CAS号 | 121264-04-8 | 分子量 | 501.83 | |
| 密度 | N/A | 沸点 | 638.9ºC at 760 mmHg | |
| 分子式 | C23H27Cl3N2O4 | 熔点 | N/A | |
| MSDS | 中文版 美版 | 闪点 | 340.2ºC |
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Teleantagonism: A pharmacodynamic property of the primary nociceptive neuron.
Proc. Natl. Acad. Sci. U. S. A. 105(49) , 19038-43, (2008) Previous work from our group showed that intrathecal (i.t.) administration of substances such as glutamate, NMDA, or PGE(2) induced sensitization of the primary nociceptive neuron (PNN hypernociception) that was inhibited by a distal intraplantar (i.pl.) inje... |
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Effects of peripherally restricted κ opioid receptor agonists on pain-related stimulation and depression of behavior in rats.
J. Pharmacol. Exp. Ther. 340(3) , 501-9, (2012) κ opioid receptor agonists that do not readily cross the blood-brain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted κ agonists have promise as candidate analgesics... |
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Peripheral kappa-opioid agonist, ICI 204448, evokes hypothermia in cold-exposed rats.
Pharmacology 74(2) , 79-83, (2005) 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, an... |
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ICI 204448: a kappa-opioid agonist with limited access to the CNS.
Br. J. Pharmacol. 96 , 986-992, (1989) 1. A number of compounds were evaluated in an attempt to identify a kappa-opioid receptor agonist with limited access to the central nervous system. 2. Quaternary derivatives of the kappa-opioid agonists tifluadom, U-50488H and ethylketocyclazocine were essen... |
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Antinociceptive effect of a kappa-opioid receptor agonist that minimally crosses the blood-brain barrier (ICI 204448) in a rat model of mononeuropathy.
Eur. J. Pharmacol. 277 , 275-280, (1995) 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... |
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Coupling of the cloned rat kappa-opioid receptor to adenylyl cyclase is dependent on receptor expression.
Neurosci. Lett. 232 , 119-122, (1997) 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 ... |
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A pharmacological profile of the novel, peripherally-selective kappa-opioid receptor agonist, EMD 61753.
Br. J. Pharmacol. 113(4) , 1317-27, (1994) 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... |
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Effects of E-2078, a stable dynorphin A(1-8) analog, on sedation and serum prolactin levels in rhesus monkeys.
Psychopharmacology 147(1) , 73-80, (1999) 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... |
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Kappa opioid agonist-induced changes in IOP: correlation with 3H-NE release and cAMP accumulation.
Exp. Eye Res. 73(2) , 167-78, (2001) Opioid receptors have been demonstrated to modulate various functions in the eye. This research project was designed to determine and compare the effects of kappa opioid agonists on selected parameters that influence ocular hydrodynamics. Experiments determin... |
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Effects of selective opioid receptor agonists and antagonists during myocardial ischaemia.
Eur. J. Pharmacol. 210(1) , 37-44, (1992) 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 cor... |