Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Adenosine Receptor Antagonists. Influence of the N5 Substituent on the Affinity at the Human A3and A2BAdenosine Receptor Subtypes:  A Molecular Modeling Investigation

2003 ◽  
Vol 46 (20) ◽  
pp. 4287-4296 ◽  
Author(s):  
Giorgia Pastorin ◽  
Tatiana Da Ros ◽  
Giampiero Spalluto ◽  
Francesca Deflorian ◽  
Stefano Moro ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Adenosine Receptor ◽  
Receptor Subtypes ◽  
Pyrimidine Derivatives ◽  
Receptor Antagonists

Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?

2002 ◽  
Vol 8 (26) ◽  
pp. 2299-2332 ◽  
Author(s):  
Pier Baraldi ◽  
Barbara Cacciari ◽  
Pier Borea ◽  
Katia Varani ◽  
Giorgia Pastorin ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Receptor Subtypes ◽  
Pyrimidine Derivatives ◽  
Receptor Antagonists

Receptors subtypes involved in adenosine-mediated modulation of norepinephrine release from cardiac nerve terminals

2004 ◽  
Vol 82 (11) ◽  
pp. 1026-1031 ◽  
Author(s):  
Mojca Lorbar ◽  
Eugene S Chung ◽  
Arash Nabi ◽  
Katarina Skalova ◽  
Richard A Fenton ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Stellate Ganglion ◽  
Receptor Subtypes ◽  
Nerve Terminals ◽  
Norepinephrine Release ◽  
Receptor Antagonists ◽  
Cardiac Nerve ◽  
Mediated Effects ◽  
Discernible Effect ◽  
Rat Hearts

The objective of this study was to determine which adenosine receptor subtypes were involved in the modulation of norepinephrine release from cardiac nerve terminals. In addition, the persistence of adenosine-mediated effects was evaluated. Rat hearts attached to the stellate ganglion were isolated and perfused. The ganglion was electrically stimulated twice (S1 and S2), allowing 10 min between the stimulations. To determine adenosine receptor subtypes, selective and nonselective adenosine agonists and antagonists were infused following S1 and until the end of S2. To evaluate the persistence of adenosine-mediated effect on norepinephrine release, the stellate ganglion was stimulated a third (S3) and fourth (S4) time. Coronary effluents were collected to determine norepinephrine content. Adenosine and a selective A1 receptor agonist, CCPA, inhibited norepinephrine release by 49% and 54%, respectively. This effect was reversed by simultaneous infusion of nonspecific (8-SPT) and specific (DPCPX) A1 receptor antagonists. Selective A2A (CGS 21680) and A3 (AB-MECA) receptor agonists had no discernible effect on norepinephrine release. Similarly, adenosine A2A receptor antagonists CSC and DMPX did not alter the dose-response relation between norepinephrine release and adenosine. Finally, the inhibitory effects of adenosine on norepinephrine release did not persist 10 min subsequent to the removal of adenosine. Adenosine inhibited norepinephrine release primarily via the adenosine A1 receptor. This effect of adenosine was of short duration. Adenosine A2A and A3 receptors were either absent or functionally insignificant in the regulation of norepinephrine release in the rat heart.Key words: adenosine, norepinephrine, receptor, rat, neurotransmitters.

Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as adenosine receptor ligands: A starting point for searching A2B adenosine receptor antagonists

2001 ◽  
Vol 53 (2-3) ◽  
pp. 225-235 ◽  
Author(s):  
Pier Giovanni Baraldi ◽  
Barbara Cacciari ◽  
Romeo Romagnoli ◽  
Karl-Norbert Klotz ◽  
Giampiero Spalluto ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Receptor Ligands ◽  
Pyrimidine Derivatives ◽  
Receptor Antagonists ◽  
A2b Adenosine Receptor ◽  
Starting Point ◽  
Adenosine Receptor Ligands

scholarly journals Structure–Activity Relationships and Molecular Modeling of 1,2,4-Triazoles as Adenosine Receptor Antagonists

2012 ◽  
Vol 3 (9) ◽  
pp. 715-720 ◽  
Author(s):  
Jens Carlsson ◽  
Dilip K. Tosh ◽  
Khai Phan ◽  
Zhan-Guo Gao ◽  
Kenneth A. Jacobson
Keyword(s):  
Molecular Modeling ◽  
Adenosine Receptor ◽  
Receptor Antagonists ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Pyrazolo Derivatives as Potent Adenosine Receptor Antagonists: An Overview on the Structure-Activity Relationships

2011 ◽  
Vol 2011 ◽  
pp. 1-15 ◽  
Author(s):  
Siew Lee Cheong ◽  
Gopalakrishnan Venkatesan ◽  
Priyankar Paira ◽  
Ramasamy Jothibasu ◽  
Alexander Laurence Mandel ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Rational Design ◽  
Receptor Subtypes ◽  
Receptor Antagonists ◽  
Design And Optimization ◽  
The Past ◽  
Chemistry Research ◽  
Pathological Conditions ◽  
Structure Activity ◽  
Selective Antagonists

In the past few decades, medicinal chemistry research towards potent and selective antagonists of human adenosine receptors (namely, A1, A2A, A2B, and A3) has been evolving rapidly. These antagonists are deemed therapeutically beneficial in several pathological conditions including neurological and renal disorders, cancer, inflammation, and glaucoma. Up to this point, many classes of compounds have been successfully synthesized and identified as potent human adenosine receptor antagonists. In this paper, an overview of the structure-activity relationship (SAR) profiles of promising nonxanthine pyrazolo derivatives is reported and discussed. We have emphasized the SAR for some representative structures such as pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidines; pyrazolo-[3,4-c] or -[4,3-c]quinolines; pyrazolo-[4,3-d]pyrimidinones; pyrazolo-[3,4-d]pyrimidines and pyrazolo-[1,5-a]pyridines. This overview not only clarifies the structural requirements deemed essential for affinity towards individual adenosine receptor subtypes, but it also sheds light on the rational design and optimization of existing structural templates to allow us to conceive new, more potent adenosine receptor antagonists.

ChemInform Abstract: 1,2,3-Triazolo(5,4-e)1,2,4-triazolo(1,5-c)pyrimidine Derivatives: A New Class of A2A Adenosine Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 27 (37) ◽  
pp. no-no
Author(s):  
P. G. BARALDI ◽  
B. CACCIARI ◽  
G. SPALLUTO ◽  
M. J. PINEDA DE LAS INFANTS ◽  
C. ZOCCHI ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Pyrimidine Derivatives ◽  
Receptor Antagonists ◽  
A2a Adenosine Receptor ◽  
New Class

Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human A1 and A2A adenosine receptor antagonists/inverse agonists

2018 ◽  
Vol 26 (12) ◽  
pp. 3688-3695 ◽  
Author(s):  
Flavia Varano ◽  
Daniela Catarzi ◽  
Matteo Falsini ◽  
Fabrizio Vincenzi ◽  
Silvia Pasquini ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Pyrimidine Derivatives ◽  
Receptor Antagonists ◽  
A2a Adenosine Receptor ◽  
Inverse Agonists
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