R,S-[3-[1-[[(3,4-二氯苯基)乙酰基]甲基]-2-(1-吡咯烷基)乙基]苯氧基]乙酸盐酸盐

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...

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...

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...

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...

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...

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 ...

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...

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...

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...

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...