Development of a lanthanide-based assay for detection of receptor–ligand interactions at the δ-opioid receptor

2005 ◽  
Vol 343 (2) ◽  
pp. 299-307 ◽  
Author(s):  
Heather L. Handl ◽  
Josef Vagner ◽  
Henry I. Yamamura ◽  
Victor J. Hruby ◽  
Robert J. Gillies
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligand ◽  
Ligand Interactions ◽  
Δ Opioid Receptor

scholarly journals In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP‐505

2018 ◽  
Vol 175 (14) ◽  
pp. 2881-2896 ◽  
Author(s):  
N Dietis ◽  
H Niwa ◽  
R Tose ◽  
J McDonald ◽  
V Ruggieri ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligand ◽  
Δ Opioid Receptor ◽  
In Vivo Characterization

A peripheral antinociceptive effects of a bifunctional μ and δ opioid receptor ligand in rat model of inflammatory bladder pain

2021 ◽  
pp. 108701
Author(s):  
Maia Terashvili ◽  
Bhavana Talluri ◽  
Watchareepohn Palangmonthip ◽  
Kenneth A. Iczkowski ◽  
Patrick Sanvanson ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Rat Model ◽  
Receptor Ligand ◽  
Bladder Pain ◽  
Antinociceptive Effects ◽  
Δ Opioid Receptor

A homogeneous single-label quenching resonance energy transfer assay for a δ-opioid receptor–ligand using intact cells

The Analyst ◽  
2013 ◽  
Vol 138 (17) ◽  
pp. 4907 ◽  
Author(s):  
Kari Kopra ◽  
Shweta ◽  
Eija Martikkala ◽  
Pekka Hänninen ◽  
Ulla Petäjä-Repo ◽  
...  
Keyword(s):  
Energy Transfer ◽  
Opioid Receptor ◽  
Resonance Energy Transfer ◽  
Resonance Energy ◽  
Intact Cells ◽  
Receptor Ligand ◽  
Δ Opioid Receptor

scholarly journals Solid-Phase Synthetic Strategy and Bioevaluation of a Labeled δ-Opioid Receptor Ligand Dmt-Tic-Lys forIn VivoImaging

2009 ◽  
Vol 11 (12) ◽  
pp. 2479-2482 ◽  
Author(s):  
Jatinder S. Josan ◽  
David L. Morse ◽  
Liping Xu ◽  
Maria Trissal ◽  
Brenda Baggett ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Solid Phase ◽  
Receptor Ligand ◽  
Synthetic Strategy ◽  
Δ Opioid Receptor

scholarly journals Structural requirements for ligands of the δ-opioid receptor

2009 ◽  
Vol 74 (11) ◽  
pp. 1207-1217 ◽  
Author(s):  
Vuk Micovic ◽  
Milovan Ivanovic ◽  
Ljiljana Dosen-Micovic
Keyword(s):  
Opioid Receptor ◽  
Binding Pocket ◽  
Hydroxyl Group ◽  
Opioid Ligands ◽  
Chiral Compounds ◽  
Alkyl Groups ◽  
Selective Ligands ◽  
Ligand Interactions ◽  
Automated Docking ◽  
Δ Opioid Receptor

The ?-opioid receptor is sensitive to ligand geometry. In order to assist the synthesis of new ?-selective opioid ligands, the structure elements of ?-selective opioid ligands necessary for their effective binding were investigated. The automated docking procedure with a flexible ligand was used to simulate the binding of 17 ?-selective ligands to the ?-receptor. It was found that voluminous N-alkyl groups reduce the binding potency of naltrindole derivatives by preventing the ligands from adopting the preferred conformation in the receptor. This was confirmed by enantiospecific binding of chiral compounds where only one enantiomer adopts the naltrindole-like preferred conformation in the binding pocket. Voluminous groups replacing the hydroxyl group in the 3-hydroxybenzyl fragment of naltrindole analogs reduce the binding potency due to unfavorable steric interactions with the receptor. The two diastereoisomers of the potent ?-opioid ligand SNC80 confirmed the preferred binding conformation and the major receptor-ligand interactions.

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