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

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.

In vitro and in vivo characterization of graphene oxide coated porcine bone granules

Carbon ◽  
2016 ◽  
Vol 103 ◽  
pp. 291-298 ◽  
Author(s):  
Valeria Ettorre ◽  
Patrizia De Marco ◽  
Susi Zara ◽  
Vittoria Perrotti ◽  
Antonio Scarano ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
In Vivo Characterization

P.3.d.011 In vitro and in vivo characterization of glycine transporter type-1 by two inhibitors, Org-24461 and NFPS

2006 ◽  
Vol 16 ◽  
pp. S435 ◽  
Author(s):  
B. Marko ◽  
G. Szabo ◽  
S. Udvari ◽  
M. Agoston ◽  
E. Szabo ◽  
...  
Keyword(s):  
Glycine Transporter ◽  
In Vivo Characterization

scholarly journals Correction to “Improving Paclitaxel Delivery: In Vitro and In Vivo Characterization of PEGylated Polyphosphoester-Based Nanocarriers”

2015 ◽  
Vol 137 (21) ◽  
pp. 6972-6972 ◽  
Author(s):  
Fuwu Zhang ◽  
Shiyi Zhang ◽  
Stephanie F. Pollack ◽  
Richen Li ◽  
Amelia M. Gonzalez ◽  
...  
Keyword(s):  
In Vivo Characterization

Synthesis, in vitro and in vivo characterization of novel 99mTc-‘4+1’-labeled 5-nitroimidazole derivatives as potential agents for imaging hypoxia

2012 ◽  
Vol 39 (5) ◽  
pp. 679-686 ◽  
Author(s):  
Javier Giglio ◽  
Soledad Fernández ◽  
Hans-Jürgen Pietzsch ◽  
Sylvia Dematteis ◽  
María Moreno ◽  
...  
Keyword(s):  
In Vivo Characterization

scholarly journals In vitro and in vivo characterization of new swine-origin H1N1 influenza viruses

Nature ◽  
2009 ◽  
Vol 460 (7258) ◽  
pp. 1021-1025 ◽  
Author(s):  
Yasushi Itoh ◽  
Kyoko Shinya ◽  
Maki Kiso ◽  
Tokiko Watanabe ◽  
Yoshihiro Sakoda ◽  
...  
Keyword(s):  
H1n1 Influenza ◽  
Influenza Viruses ◽  
In Vivo Characterization

In vivo characterization of estrogen receptor modulators with reduced genomic versus nongenomic activity in vitro

2008 ◽  
Vol 111 (1-2) ◽  
pp. 95-100 ◽  
Author(s):  
Christiane Otto ◽  
Iris Fuchs ◽  
Helga Altmann ◽  
Mario Klewer ◽  
Gilda Schwarz ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Modulators ◽  
In Vivo Characterization ◽  
Receptor Modulators

In vitro and in vivo characterization of PheTQS, a novel α7 nAChR positive allosteric modulator

2009 ◽  
Vol 78 (7) ◽  
pp. 913 ◽  
Author(s):  
James N.C. Kew ◽  
Selina Mok ◽  
Annette Weil ◽  
Caterina Virginio ◽  
Laura Castelletti ◽  
...  
Keyword(s):  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Α7 Nachr ◽  
In Vivo Characterization
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