Related Experiment Video
Updated: Feb 26, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
Published on: June 7, 2016
AT2 receptors in cardiovascular and renal diseases
Elena Kaschina1, Pawel Namsolleck2, Thomas Unger2
1Charité - Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, Institute of Pharmacology, Center for Cardiovascular Research (CCR), Germany.
Abstract:
The renin-angiotensin system (RAS) plays an important role in the initiation and progression of cardiovascular and renal diseases. These actions mediated by AT1 receptor (AT1R) are well established and led to development of selective AT1R blockers (ARBs). In contrast, there is scientific evidence that AT2 receptor (AT2R) mediates effects different from and often opposing those of the AT1R. Meagrely expressed in healthy tissue the AT2R is upregulated in injuries providing an endogenous protection to inflammatory, oxidative and apoptotic processes. Interestingly the beneficial effects mediated by AT2R can be further enhanced by pharmacological intervention using the recently developed AT2R agonists. This review article summarizes our current knowledge about regulation, signalling and effects mediated by AT2R in health and disease, with emphasis on cardiac and renal systems. At the end a novel concept of natural protective systems will be introduced and discussed as an attractive target in drug development.
Insights
The angiotensin II type 2 receptor (AT2R) offers protective effects against cardiovascular and renal diseases, opposing the AT1 receptor. AT2R agonists enhance these natural protective mechanisms, presenting a new drug development target.
Area of Science:
- Cardiovascular and Renal Medicine
- Pharmacology
- Molecular Biology
Background:
- The renin-angiotensin system (RAS) is implicated in cardiovascular and renal diseases.
- Angiotensin II type 1 receptor blockers (ARBs) target the pro-disease effects of AT1R.
- Emerging evidence highlights the protective roles of the angiotensin II type 2 receptor (AT2R), often opposing AT1R actions.
Purpose of the Study:
- To review the regulation, signaling, and effects of AT2R in health and disease.
- To emphasize AT2R's role in cardiac and renal systems.
- To introduce a novel concept of natural protective systems as drug targets.
Main Methods:
- Literature review of scientific evidence on AT2R.
- Analysis of AT2R expression and function in physiological and pathological conditions.
- Discussion of AT2R agonists and their therapeutic potential.
Main Results:
- AT2R is upregulated during injury and mediates protective effects against inflammation, oxidative stress, and apoptosis.
- AT2R activation provides benefits often counteracting AT1R-mediated damage.
- Pharmacological enhancement of AT2R activity shows therapeutic promise.
Conclusions:
- AT2R represents a significant endogenous protective system in cardiovascular and renal health.
- Targeting AT2R, particularly with agonists, offers a promising therapeutic strategy.
- Natural protective systems mediated by AT2R are attractive targets for future drug development.
Related Concept Videos
Antihypertensive Drugs: Angiotensin II Receptor Blockers
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Antihypertensive Drugs: Action of β1 Blockers
Adrenergic Receptors: ɑ Subtype
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
Antihypertensive Drugs: Direct Renin Inhibitors

