Synthesis and Characterization of Novel 2-Amino-3-benzoylthiophene Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine A1 Receptor

2012 ◽  
Vol 55 (5) ◽  
pp. 2367-2375 ◽  
Author(s):  
Celine Valant ◽  
Luigi Aurelio ◽  
Shane M. Devine ◽  
Trent D. Ashton ◽  
Jonathan M. White ◽  
...  
Keyword(s):  
Adenosine A1 Receptor ◽  
Synthesis And Characterization ◽  
Adenosine A1 ◽  
A1 Receptor

Characterization of adenosine A1 receptor in cultured myoblast C2C12 cells of mice

2001 ◽  
Vol 87 (1) ◽  
pp. 59-64 ◽  
Author(s):  
I-Min Liu ◽  
Tung-Yuan Lai ◽  
Chin-Chuan Tsai ◽  
Juei-Tang Cheng
Keyword(s):  
Adenosine A1 Receptor ◽  
C2c12 Cells ◽  
Adenosine A1 ◽  
A1 Receptor

Reaction Pathways to 2-Aminothiophenes and Thiophene-3-carbonitriles

2009 ◽  
Vol 62 (5) ◽  
pp. 402 ◽  
Author(s):  
Luigi Aurelio ◽  
Bernard L. Flynn ◽  
Peter J. Scammells
Keyword(s):  
Comparative Studies ◽  
Reaction Pathway ◽  
Reaction Pathways ◽  
Synthesis And Characterization ◽  
The Past ◽  
Adenosine A1 ◽  
Unexpected Reaction ◽  
Potential Applications ◽  
A1 Receptor

Over the past two decades 2-amino-3-benzoylthiophenes have been found to act as allosteric enhancers of the adenosine A1 receptor (A1AR). As such, compounds of this type have potential applications in the therapy of a variety of disorders by enhancing A1AR activation. Initial studies in this field identified various 2-amino-3-benzoylthiophenes as potential leads and of these PD 81723 1a has become the benchmark for comparative studies due to its favourable ratio of allosteric enhancement to antagonism. Surprisingly the synthesis and characterization of PD 81723 1a has not been previously reported. Herein we report the synthesis and characterization of this important A1AR allosteric enhancer. As part of this study we also found an unexpected reaction pathway to 2-phenylthiophene-3-carbonitriles.

scholarly journals Identification and characterization of adenosine A1 receptor-cAMP system in human glomeruli

1993 ◽  
Vol 43 (4) ◽  
pp. 928-932 ◽  
Author(s):  
Yoshiyuki Toya ◽  
Satoshi Umemura ◽  
Tamio Iwamoto ◽  
Nobuhito Hirawa ◽  
Minoru Kihara ◽  
...  
Keyword(s):  
Adenosine A1 Receptor ◽  
Adenosine A1 ◽  
A1 Receptor ◽  
Camp System ◽  
Identification And Characterization

scholarly journals Characterization of Adenosine-A1 Receptor-Mediated Antilipolysis in Rats by Tissue Microdialysis, 1H-Spectroscopy, and Glucose Clamp Studies

Diabetes ◽  
2004 ◽  
Vol 53 (7) ◽  
pp. 1920-1926 ◽  
Author(s):  
C. Schoelch ◽  
J. Kuhlmann ◽  
M. Gossel ◽  
G. Mueller ◽  
C. Neumann-Haefelin ◽  
...  
Keyword(s):  
Glucose Clamp ◽  
Adenosine A1 Receptor ◽  
Adenosine A1 ◽  
A1 Receptor

scholarly journals Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor

2010 ◽  
Vol 80 (8) ◽  
pp. 1180-1189 ◽  
Author(s):  
J. Robert Lane ◽  
Elisabeth Klaasse ◽  
Judy Lin ◽  
John van Bruchem ◽  
Margot W. Beukers ◽  
...  
Keyword(s):  
Adenosine A1 Receptor ◽  
High Affinity ◽  
Adenosine A1 ◽  
A1 Receptor
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