The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma

2005 ◽  
Vol 15 (3) ◽  
pp. 609-612 ◽  
Author(s):  
Jeff Zablocki ◽  
Rao Kalla ◽  
Thao Perry ◽  
Venkata Palle ◽  
Vaibhav Varkhedkar ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Potential Treatment ◽  
A2b Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
High Affinity

Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes

2016 ◽  
Vol 59 (5) ◽  
pp. 1967-1983 ◽  
Author(s):  
Abdelaziz El Maatougui ◽  
Jhonny Azuaje ◽  
Manuel González-Gómez ◽  
Gabriel Miguez ◽  
Abel Crespo ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A2b Adenosine Receptor ◽  
Adenosine Receptor Antagonist

Abstract 5555:In vivoandin vitrocharacterization of RVU330 best-in-class dual A2A/A2B adenosine receptor antagonist

2020 ◽  
Author(s):  
Michał Gałęzowski ◽  
Katarzyna Dziedzic ◽  
Paulina Węgrzyn ◽  
Aniela Gołas ◽  
Magdalena Bońkowska ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A2b Adenosine Receptor ◽  
Adenosine Receptor Antagonist

scholarly journals Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist

2010 ◽  
Vol 2 (3) ◽  
pp. 213-218 ◽  
Author(s):  
Paul Eastwood ◽  
Cristina Esteve ◽  
Jacob González ◽  
Silvia Fonquerna ◽  
Josep Aiguadé ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
A2b Adenosine Receptor ◽  
Adenosine Receptor Antagonist

Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity

1999 ◽  
Vol 48 (3) ◽  
pp. 95-103 ◽  
Author(s):  
Maarten de Zwart ◽  
Roel C. Vollinga ◽  
Margot W. Beukers ◽  
Danielle F. Sleegers ◽  
Jacobien K. von Frijtag Drabbe K�nzel ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Adenosine Receptor ◽  
Adenosine A2b Receptor ◽  
Adenosine Receptor Antagonist ◽  
High Affinity ◽  
A2b Receptor ◽  
Derivatives Of ◽  
Adenosine A2b

scholarly journals Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers

2013 ◽  
Vol 11 (34) ◽  
pp. 5673 ◽  
Author(s):  
Andrea J. Vernall ◽  
Leigh A. Stoddart ◽  
Stephen J. Briddon ◽  
Hui Wen Ng ◽  
Charles A. Laughton ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Fluorescent Probes ◽  
Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
High Affinity

CPX, a selective A1-adenosine-receptor antagonist, regulates intracellular pH in cystic fibrosis cells

1995 ◽  
Vol 269 (1) ◽  
pp. C226-C233 ◽  
Author(s):  
V. Casavola ◽  
R. J. Turner ◽  
C. Guay-Broder ◽  
K. A. Jacobson ◽  
O. Eidelman ◽  
...  
Keyword(s):  
Cystic Fibrosis ◽  
Receptor Antagonist ◽  
Intracellular Ph ◽  
Adenosine Receptor ◽  
Ph Regulation ◽  
Cystic Fibrosis Transmembrane Regulator ◽  
Wild Type ◽  
A1 Adenosine Receptor ◽  
Adenosine Receptor Antagonist ◽  
Cystic Fibrosis Transmembrane

The selective A1-adenosine-receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (CPX), has been reported to activate Cl- efflux from cystic fibrosis cells, such as pancreatic CFPAC-1 and lung IB3 cells bearing the cystic fibrosis transmembrane regulator(delta F508) mutation, but has little effect on the same process in cells repaired by transfection with wild-type cystic fibrosis transmembrane regulator (O. Eidelman, C. Guay-Broder, P. J. M. van Galen, K. A. Jacobson, C. Fox, R. J. Turner, Z. I. Cabantchik, and H. B. Pollard. Proc. Natl. Acad. Sci. USA 89: 5562-5566, 1992). We report here that CPX downregulates Na+/H+ exchange activity in CFPAC-1 cells but has a much smaller effect on cells repaired with the wild-type gene. CPX also mildly decreases resting intracellular pH. In CFPAC-1 cells, this downregulation is dependent on the presence of adenosine, since pretreatment of the cells with adenosine deaminase blocks the CPX effect. We also show that, by contrast, CPX action on these cells does not lead to alterations in intracellular free Ca2+ concentration. We conclude that CPX affects pH regulation in CFPAC-1 cells, probably by antagonizing the tonic action of endogenous adenosine.

Sign in / Sign up

Export Citation Format

Share Document