scholarly journals Effects of P1 and P2 receptor antagonists on β,γ -methyleneATP- and CGS21680-induced cyclic AMP formation in NG108-15 cells

2000 ◽  
Vol 129 (2) ◽  
pp. 291-298 ◽  
Author(s):  
Satoko Ohkubo ◽  
Junko Kimura ◽  
Hironori Nakanishi ◽  
Isao Matsuoka
Keyword(s):  
Cyclic Amp ◽  
P2 Receptor ◽  
Receptor Antagonists

Potential Therapeutic Applications of P2 Receptor Antagonists: From Bench to Clinical Trials

2019 ◽  
Vol 20 (9) ◽  
pp. 919-937 ◽  
Author(s):  
Natiele C. da Silva Ferreira ◽  
Luiz A. Alves ◽  
Rômulo J. Soares-Bezerra
Keyword(s):  
Clinical Trials ◽  
P2 Receptors ◽  
Experimental Models ◽  
New Drugs ◽  
Receptor Subtype ◽  
P2 Receptor ◽  
Receptor Antagonists ◽  
Purines And Pyrimidines

Background: Extracellular purines and pyrimidines have important physiological functions in mammals. Purines and pyrimidines act on P1 and P2 purinergic receptors, which are widely expressed in the plasma membrane in various cell types. P2 receptors act as important therapeutic targets and are associated with several disorders, such as pain, neurodegeneration, cancer, inflammation, and thrombosis. However, the use of antagonists for P2 receptors in clinical therapy, with the exception of P2Y12, is a great challenge. Currently, many research groups and pharmaceutical companies are working on the development of specific antagonist molecules for each receptor subtype that could be used as new medicines to treat their respective disorders. Objective: The present review compiles some interesting findings on the application of P2 receptor antagonists in different in vitro and in vivo experimental models as well as the progress of advanced clinical trials with these compounds. Conclusion: Despite all of the exciting results obtained on the bench, few antagonists of P2 receptors advanced to the clinical trials, and once they reach this stage, the effectiveness of the therapy is not guaranteed, as in the example of P2X7 antagonists. Despite this, P2Y12 receptor antagonists have a history of success and have been used in therapy for at least two decades to prevent thrombosis in patients at risk for myocardial infarctions. This breakthrough is the motivation for scientists to develop new drugs with antagonistic activity for the other P2 receptors; thus, in a matter of years, we will have an evolution in the field of purinergic therapy.

Structure-Activity Relationships of Suramin and Pyridoxal-5-phosphate Derivatives as P2 Receptor Antagonists

2002 ◽  
Vol 8 (26) ◽  
pp. 2371-2399 ◽  
Author(s):  
Gunter Lambrecht ◽  
Kirsten Braun ◽  
Susanne Damer ◽  
Matthias Ganso ◽  
Caren Hildebrandt ◽  
...  
Keyword(s):  
P2 Receptor ◽  
Receptor Antagonists ◽  
Structure Activity Relationships ◽  
Structure Activity

Inhibition of human and mouse plasma membrane bound NTPDases by P2 receptor antagonists

2007 ◽  
Vol 74 (10) ◽  
pp. 1524-1534 ◽  
Author(s):  
Mercedes N. Munkonda ◽  
Gilles Kauffenstein ◽  
Filip Kukulski ◽  
Sébastien A. Lévesque ◽  
Charlène Legendre ◽  
...  
Keyword(s):  
Plasma Membrane ◽  
P2 Receptor ◽  
Receptor Antagonists ◽  
Mouse Plasma ◽  
Membrane Bound ◽  
Human And Mouse

P2-receptor antagonists: IV. Blockade of P2-receptor subtypes and ecto-nucleotidases by compounds related to reactive blue 2

1998 ◽  
Vol 357 (2) ◽  
pp. 111-120 ◽  
Author(s):  
Florin Tuluc ◽  
R. Bültmann ◽  
Markus Glänzel ◽  
August Wilhelm Frahm ◽  
Klaus Starke
Keyword(s):  
Receptor Subtypes ◽  
P2 Receptor ◽  
Receptor Antagonists ◽  
Reactive Blue 2

scholarly journals Pharmacological profile of a novel cyclic AMP-linked P2 receptor on undifferentiated HL-60 leukemia cells

1998 ◽  
Vol 124 (7) ◽  
pp. 1580-1585 ◽  
Author(s):  
Arthur D. Conigrave ◽  
Joanne Y. Lee ◽  
Louise Van Der Weyden ◽  
Lele Jiang ◽  
Peter Ward ◽  
...  
Keyword(s):  
Cyclic Amp ◽  
Leukemia Cells ◽  
P2 Receptor ◽  
Pharmacological Profile
Sign in / Sign up

Export Citation Format

Share Document