Substituted pyrazolo[3,4-b]pyridines as human A1 adenosine antagonists: Developments in understanding the receptor stereoselectivity

2011 ◽  
Vol 9 (12) ◽  
pp. 4448 ◽  
Author(s):  
Tiziano Tuccinardi ◽  
Alessandra Tania Zizzari ◽  
Chiara Brullo ◽  
Simona Daniele ◽  
Francesca Musumeci ◽  
...  
Keyword(s):  
Adenosine Antagonists

Effects of adenosine antagonists on hexose uptake and preconditioning in perfused rat heart

1993 ◽  
Vol 265 (4) ◽  
pp. C1146-C1155 ◽  
Author(s):  
E. Murphy ◽  
T. A. Fralix ◽  
R. E. London ◽  
C. Steenbergen
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Magnetic Resonance ◽  
Beneficial Effect ◽  
Recovery Of Function ◽  
Anaerobic Glycolysis ◽  
Perfused Rat Heart ◽  
Adenosine Antagonists ◽  
Adenosine Antagonist ◽  
Ionic Changes ◽  
Hexose Uptake

Preconditioning with brief intermittent periods of ischemia has been shown to lessen the detrimental effects of a subsequent sustained (30-60 min) period of ischemia. Because adenosine has been suggested to be the mediator of preconditioning, we were interested in investigating whether adenosine antagonists would block the effect of preconditioning on ionic changes during ischemia. We found that 10 microM of the adenosine antagonist BW-A1433U did not reverse the effect of preconditioning on intracellular pH (pHi). Hearts preconditioned with BW-A1433U had virtually no decrease in pHi during the 30-min sustained period of ischemia; after 30 min of ischemia, the pH in untreated hearts was 5.97 +/- 0.16 compared with 6.52 +/- 0.10 in preconditioned hearts and 6.90 +/- 0.08 in hearts preconditioned plus BW-A1433U. Because anaerobic glycolysis is largely responsible for the fall in pHi during ischemia, we examined the effect of BW-A1433U [and other adenosine antagonists, such as PD-115,199 and 8-cyclopentyl-1,3-dipropylxanthine (CPDPX)] on glucose uptake and phosphorylation during aerobic perfusion using 31P-nuclear magnetic resonance to monitor uptake and phosphorylation of 2-deoxyglucose (2-DG) to 2-deoxyglucose 6-phosphate (2-DG-6-P) when one-half of the glucose in the perfusate was replaced with 2-DG. Uptake of 2-DG-6-P after 15 min was reduced by 66% in the presence of BW-A1433U and 82% in the presence of PD-115,199 as compared with untreated hearts, but was not reduced in the presence of CPDPX. Thus CPDPX was the only adenosine antagonist tested that did not block accumulation of 2-DG-6-P. We also found that CPDPX did not block the beneficial effect of preconditioning on ionic alterations during a sustained 30-min period of ischemia or the improved recovery of function on reflow.

1H-Imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists

1991 ◽  
Vol 34 (3) ◽  
pp. 1202-1206 ◽  
Author(s):  
Philip J. M. Van Galen ◽  
Peter Nissen ◽  
Ineke Van Wijngaarden ◽  
Adriaan P. Ijzerman ◽  
Willem Soudijn
Keyword(s):  
Adenosine Antagonists

Adenosine antagonists

1985 ◽  
Vol 24 (7) ◽  
pp. 635-638 ◽  
Author(s):  
Susan R.B. Weiss ◽  
R.M. Post ◽  
P.J. Marangos ◽  
Jitendra Patel
Keyword(s):  
Adenosine Antagonists

scholarly journals Activation of the N-Methyl-D-Aspartate (NMDA) Receptor by Adenosine Antagonists in Brain Cell Membranes of Newborn Piglets

1999 ◽  
Vol 45 (4, Part 2 of 2) ◽  
pp. 68A-68A
Author(s):  
Peter J Marro ◽  
Juan R Ballesteros ◽  
Anli Zhu ◽  
Om P Mishra ◽  
Maria Delivoria-Papadopoulos
Keyword(s):  
Nmda Receptor ◽  
Cell Membranes ◽  
Brain Cell ◽  
Adenosine Antagonists ◽  
Newborn Piglets

Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists

1993 ◽  
Vol 36 (10) ◽  
pp. 1333-1342 ◽  
Author(s):  
Kenneth A. Jacobson ◽  
Carola Gallo-Rodriguez ◽  
Neli Melman ◽  
Bilha Fischer ◽  
Michel Maillard ◽  
...  
Keyword(s):  
Adenosine Antagonists ◽  
Structure Activity Relationships ◽  
Structure Activity
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