Design, Synthesis and Evaluation of Highly Selective AT2R Agonists

High blood pressure is caused by the hormone angiotensin II and can lead to severe damage to the heart and other organs, called fibrosis. High blood pressure is often treated by blocking the angiotensin type 1 receptor (AT1R) but this cannot reverse fibrosis. By comparison, stimulation of the angiotensin type 2 receptor (AT2R) can reverse fibrosis, but there are very few such compounds. This Thesis used a novel approach to develop several lead compounds which bound strongly only to AT2R and showed long-lasting anti-fibrotic effects. This research now provides the basis for future drug development for the treatment of fibrosis.