scholarly journals Adenosine A2A receptor modulates vascular response in soluble epoxide hydrolase‐null mice through cyp2j‐epoxygenases and PPARγ

2013 ◽  
Vol 27 (S1) ◽  
Author(s):  
Mohammed A Nayeem ◽  
Isha Pradhan ◽  
S Jamal Mustafa ◽  
Christophe Morisseau ◽  
John R Falck ◽  
...  
Keyword(s):  
Epoxide Hydrolase ◽  
Soluble Epoxide Hydrolase ◽  
Adenosine A2a Receptor ◽  
Vascular Response ◽  
A2a Receptor ◽  
Adenosine A2a

scholarly journals Disruption of soluble epoxide hydrolase modulates adenosine‐induced response: role of adenosine A2A receptor and cyp‐epoxygenases

2012 ◽  
Vol 26 (S1) ◽  
Author(s):  
Mohammed A. Nayeem ◽  
Darryl C. Zeldin ◽  
Isha Pradhan ◽  
S Jamal Mustafa ◽  
John R. Falck ◽  
...  
Keyword(s):  
Epoxide Hydrolase ◽  
Soluble Epoxide Hydrolase ◽  
Adenosine A2a Receptor ◽  
Induced Response ◽  
A2a Receptor ◽  
Adenosine A2a

scholarly journals Modulation of vascular response by high salt intake depends on the presence or absence of adenosine A2A receptor using A2A AR‐null mice

2013 ◽  
Vol 27 (S1) ◽  
Author(s):  
Isha Pradhan ◽  
Jamal S Mustafa ◽  
Darryl C Zeldin ◽  
Catherine Ledent ◽  
John R Falck ◽  
...  
Keyword(s):  
Salt Intake ◽  
Adenosine A2a Receptor ◽  
High Salt ◽  
Vascular Response ◽  
High Salt Intake ◽  
A2a Receptor ◽  
Adenosine A2a

Synthesis of the Adenosine A2A Receptor Fluorescent Agonist MRS5424

BIO-PROTOCOL ◽  
2014 ◽  
Vol 4 (6) ◽  
Author(s):  
Kenneth Jacobson ◽  
Francisco Ciruela
Keyword(s):  
Adenosine A2a Receptor ◽  
A2a Receptor ◽  
Adenosine A2a

Optimization of the Human Adenosine A2a Receptor Yields in Saccharomyces cerevisiae

2008 ◽  
Vol 22 (5) ◽  
pp. 1249-1255 ◽  
Author(s):  
Alison Wedekind ◽  
Michelle A. O'Malley ◽  
Ronald T. Niebauer ◽  
Anne S. Robinson
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Adenosine A2a Receptor ◽  
A2a Receptor ◽  
Adenosine A2a

scholarly journals A Cellular Assay for the Identification and Characterization of Connexin Gap Junction Modulators

2021 ◽  
Vol 22 (3) ◽  
pp. 1417
Author(s):  
Azeem Danish ◽  
Robin Gedschold ◽  
Sonja Hinz ◽  
Anke C. Schiedel ◽  
Dominik Thimm ◽  
...  
Keyword(s):  
Gap Junctions ◽  
Small Molecules ◽  
High Throughput Screening ◽  
Cell Communication ◽  
Receptor Activation ◽  
Adenosine A2a Receptor ◽  
Intracellular Camp ◽  
Donor Cells ◽  
A2a Receptor ◽  
Adenosine A2a

Connexin gap junctions (Cx GJs) enable the passage of small molecules and ions between cells and are therefore important for cell-to-cell communication. Their dysfunction is associated with diseases, and small molecules acting as modulators of GJs may therefore be useful as therapeutic drugs. To identify GJ modulators, suitable assays are needed that allow compound screening. In the present study, we established a novel assay utilizing HeLa cells recombinantly expressing Cx43. Donor cells additionally expressing the Gs protein-coupled adenosine A2A receptor, and biosensor cells expressing a cAMP-sensitive GloSensor luciferase were established. Adenosine A2A receptor activation in the donor cells using a selective agonist results in intracellular cAMP production. The negatively charged cAMP migrates via the Cx43 gap junctions to the biosensor cells and can there be measured by the cAMP-dependent luminescence signal. Cx43 GJ modulators can be expected to impact the transfer of cAMP from the donor to the biosensor cells, since cAMP transit is only possible via GJs. The new assay was validated by testing the standard GJ inhibitor carbenoxolon, which showed a concentration-dependent inhibition of the signal and an IC50 value that was consistent with previously reported values. The assay was demonstrated to be suitable for high-throughput screening.

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