Methylated Analogues of Methyl (R)-4-(3,4-Dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as Highly Potent κ-Receptor Agonists:  Stereoselective Synthesis, Opioid-Receptor Affinity, Receptor Selectivity, and Functional Studies

2001 ◽  
Vol 44 (17) ◽  
pp. 2814-2826 ◽  
Author(s):  
Stella Soukara ◽  
Christoph A. Maier ◽  
Ursula Predoiu ◽  
Andreas Ehret ◽  
Rolf Jackisch ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Stereoselective Synthesis ◽  
Receptor Selectivity ◽  
Receptor Affinity ◽  
Receptor Agonists ◽  
Functional Studies ◽  
Affinity Receptor ◽  
Κ Receptor

Conformationally Constrained κ Receptor Agonists: Stereoselective Synthesis and Pharmacological Evaluation of 6,8-Diazabicyclo[3.2.2]nonane Derivatives†

2010 ◽  
Vol 53 (10) ◽  
pp. 4212-4222 ◽  
Author(s):  
Christian Geiger ◽  
Christel Zelenka ◽  
Kirstin Lehmkuhl ◽  
Dirk Schepmann ◽  
Werner Englberger ◽  
...  
Keyword(s):  
Stereoselective Synthesis ◽  
Conformationally Constrained ◽  
Receptor Agonists ◽  
Pharmacological Evaluation ◽  
Κ Receptor

Effects of polar κ receptor agonists designed for the periphery on ATP-induced Ca2+ release from keratinocytes

MedChemComm ◽  
2016 ◽  
Vol 7 (2) ◽  
pp. 317-326 ◽  
Author(s):  
Fabian Galla ◽  
Christian Bourgeois ◽  
Kirstin Lehmkuhl ◽  
Dirk Schepmann ◽  
Michael Soeberdt ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Human Keratinocytes ◽  
Receptor Agonists ◽  
Opioid Receptor Agonist ◽  
Κ Receptor

The very polar pyridylmethyl derivative 5a (log D7.4 = 1.1) represents a potent and selective full κ-opioid receptor agonist (Ki = 0.13 nM, EC50 = 33 nM), which reduced the release of Ca2+-ions into the cytoplasm in human keratinocytes.

Kappa Opioid Receptor Inhibition of Glutamatergic Transmission in the Nucleus Accumbens Shell

2001 ◽  
Vol 85 (3) ◽  
pp. 1153-1158 ◽  
Author(s):  
Gregory O. Hjelmstad ◽  
Howard L. Fields
Keyword(s):  
Nucleus Accumbens ◽  
Synaptic Transmission ◽  
Opioid Receptor ◽  
Receptor Activation ◽  
Kappa Opioid Receptor ◽  
Excitatory Synaptic Transmission ◽  
Nucleus Accumbens Shell ◽  
Receptor Agonists ◽  
Κ Receptor

Microinjection of κ-opioid receptor agonists into the nucleus accumbens produces conditioned place aversion. While attention has focused primarily on the inhibition of dopamine release by κ-receptor agonists as the synaptic mechanism underlying this effect, recent anatomical studies have raised the possibility that regulation of noncatecholaminergic transmission also contribute. We have investigated the effects of κ-receptor activation on fast excitatory synaptic transmission in an in vitro slice preparation using whole cell voltage-clamp or extracellular field recordings in the shell region of the nucleus accumbens. The κ-receptor agonist U69593 produces a pronounced, dose-dependent inhibition of glutamatergic excitatory postsynaptic currents (EPSCs) that can be reversed by 100 nM nor-BNI. Furthermore, U69593 causes an increase in the paired-pulse ratio as well as a decrease in the frequency of spontaneous miniature events, suggesting a presynaptic site of action. Despite anatomical evidence for κ-receptor localization on dendritic spines of nucleus accumbens neurons, no electrophysiological evidence of a postsynaptic effect was found. This presynaptic inhibition of excitatory synaptic transmission in the nucleus accumbens shell provides a novel mechanism that may contribute to the κ-receptor–mediated aversion observed in intact animals.

scholarly journals Cover Feature: Synthesis and Assessment of Fused β‐Carboline Derivatives as Kappa Opioid Receptor Agonists (12/2021)

ChemMedChem ◽  
2021 ◽  
Vol 16 (12) ◽  
pp. 1834-1834
Author(s):  
Veena D. Yadav ◽  
Lalan Kumar ◽  
Poonam Kumari ◽  
Sakesh Kumar ◽  
Maninder Singh ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

scholarly journals The region in the μ opioid receptor conferring selectivity for sufentanil over the δ receptor is different from that over the κ receptor

FEBS Letters ◽  
1996 ◽  
Vol 384 (2) ◽  
pp. 198-202 ◽  
Author(s):  
Jinmin Zhu ◽  
Ji-Chun Xue ◽  
Ping-Yee Law ◽  
Patricia A. Claude ◽  
Lai-Yi Luo ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Μ Opioid Receptor ◽  
Κ Receptor

Opioid receptor affinity of multivalent ligand system consisting of polymerized liposome

2009 ◽  
Vol 48 (1) ◽  
pp. 95-101 ◽  
Author(s):  
SHOKO TETSUI ◽  
JINBAO ZHAO ◽  
SHUNSAKU KIMURA ◽  
YUKIO IMANISHI
Keyword(s):  
Opioid Receptor ◽  
Receptor Affinity ◽  
Ligand System
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