Immunofluorescence analysis of antisense oligodeoxynucleotide-mediated ‘knock-down’ of the mouse δ opioid receptor in vitro and in vivo

1996 ◽  
Vol 213 (3) ◽  
pp. 205-208
Author(s):  
Josephine Lai ◽  
Maureen Riedl ◽  
Laura S. Stone ◽  
Ulf Arvidsson ◽  
Edward J. Bilsky ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Antisense Oligodeoxynucleotide ◽  
Immunofluorescence Analysis ◽  
Knock Down ◽  
Δ Opioid Receptor

scholarly journals Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7236
Author(s):  
Yazan J. Meqbil ◽  
Hongyu Su ◽  
Robert J. Cassell ◽  
Kendall L. Mores ◽  
Anna M. Gutridge ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Clinical Drug Development ◽  
In Vitro Characterization ◽  
Opioid Receptor Agonist ◽  
Negative Allosteric Modulator ◽  
Δ Opioid Receptor ◽  
Clinical Drug

The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed. It has increasingly become apparent that the SNC80 scaffold carries with it potent and efficacious β-arrestin recruitment. Here, we screened a relatively small (5120 molecules) physical drug library to identify δOR agonists that underrecruit β-arrestin, as it has been suggested that compounds that efficaciously recruit β-arrestin are proconvulsant. The screen identified a hit compound and further characterization using cellular binding and signaling assays revealed that this molecule (R995045, compound 1) exhibited ten-fold selectivity over µ- and κ-opioid receptors. Compound 1 represents a novel chemotype at the δOR. A subsequent characterization of fourteen analogs of compound 1, however did not identify a more potent δOR agonist. Computational modeling and in vitro characterization of compound 1 in the presence of the endogenous agonist leu-enkephalin suggest compound 1 may also bind allosterically and negatively modulate the potency of Leu-enkephalin to inhibit cAMP, acting as a ‘NAM-agonist’ in this assay. The potential physiological utility of such a class of compounds will need to be assessed in future in vivo assays.

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

In Vitro and In Vivo Metabolism of a Selective δ-Opioid Receptor

2011 ◽  
Vol 39 (10) ◽  
pp. 1883-1894 ◽  
Author(s):  
Jian Guo ◽  
Chungang Gu ◽  
Diansong Zhou ◽  
Charles S. Elmore ◽  
Khanh H. Bui ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
In Vivo Metabolism ◽  
Δ Opioid Receptor

scholarly journals Upregulation of the δ opioid receptor in liver cancer promotes liver cancer progression both in vitro and in vivo

2013 ◽  
Vol 43 (4) ◽  
pp. 1281-1290 ◽  
Author(s):  
BO TANG ◽  
YANG LI ◽  
SHENGGUANG YUAN ◽  
STEPHEN TOMLINSON ◽  
SONGQING HE
Keyword(s):  
Liver Cancer ◽  
Opioid Receptor ◽  
Cancer Progression ◽  
Δ Opioid Receptor

δ Opioid Receptor Inverse Agonists and their In Vivo Pharmacological Effects

2020 ◽  
Vol 20 (31) ◽  
pp. 2889-2902 ◽  
Author(s):  
Shigeto Hirayama ◽  
Hideaki Fujii
Keyword(s):  
Opioid Receptor ◽  
Short Term Memory ◽  
Inverse Agonist ◽  
Pharmacological Effects ◽  
Short Term ◽  
Inverse Agonists ◽  
Δ Opioid Receptor ◽  
Receptor Inverse Agonist

The discovery of δ opioid receptor inverse agonist activity induced by ICI-174,864, which was previously reported as an δ opioid receptor antagonist, opened the door for the investigation of inverse agonism/constitutive activity of the receptors. Various peptidic or non-peptidic δ opioid receptor inverse agonists have since been developed. Compared with the reports dealing with in vitro inverse agonist activities of novel compounds or known compounds as antagonists, there have been almost no publications describing the in vivo pharmacological effects induced by a δ opioid receptor inverse agonist. After the observation of anorectic effects with the δ opioid receptor antagonism was discussed in the early 2000s, the short-term memory improving effects and antitussive effects have been very recently reported as possible pharmacological effects induced by a δ opioid receptor inverse agonist. In this review, we will survey the developed δ opioid receptor inverse agonists and summarize the possible in vivo pharmacological effects by δ opioid receptor inverse agonists. Moreover, we will discuss important issues involved in the investigation of the in vivo pharmacological effects produced by a δ opioid receptor inverse agonist.

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