CGP42112: the full AT2 receptor agonist and its role in the renin-angiotensin-aldosterone system: no longer misunderstood
Document Type
Article
Publication Date
11-11-2022
Publication Title
Clinical Science
Keywords
AT2R, Antagonist, CGP42112, Full Agonist, Partial Agonist
ISSN
0143-5221
Volume
136
Issue/No.
21
First Page
1513
Last Page
1533
Abstract
For years, the AT2R-selective ligand CGP42112 has been erroneously characterized as a partial agonist, partly due to its ability to also interact with the AT1R at high concentrations. As late as 2009, it was still being characterized as an antagonist as well. In this perspective/opinion piece, we try to resolve the ambiguity that surrounds the efficacy of this compound by extensively reviewing the literature, tracing its beginnings to 1989, showing that CGP42112 has never been convincingly shown to be a partial agonist or an antagonist at the AT2R. While CGP42112 is now routinely characterized as an AT2R agonist, regrettably, there is a paucity of studies that can validate its efficacy as a full agonist at the AT2R, leaving the door open for continuing speculation regarding the extent of its efficacy. Hopefully, the information presented in this perspective/opinion piece will firmly establish CGP42112 as a full agonist at the AT2R such that it can once again be used as a tool to study the AT2R.
NSUWorks Citation
Restrepo, Yazmin M.; Noto, Natalia M.; and Speth, Robert C., "CGP42112: the full AT2 receptor agonist and its role in the renin-angiotensin-aldosterone system: no longer misunderstood" (2022). HPD Articles. 37.
https://nsuworks.nova.edu/hpd_facarticles/37
ORCID ID
0000-0002-6434-2140
DOI
10.1042/CS20220261
Copyright
© 2022 The Author(s).
