Determination of the ligand pharmacophore required for secondary conformation activation of the human Beta1-adrenoceptor

This thesis aims to better understand at the cellular level the behaviour of beta-blockers, which decrease the heart rate and are used daily in the treatment of cardiovascular diseases and anxiety. Some medicines in this class can both decrease and increase the heart rate depending on the amount used. To study this, we developed new molecules based on a known beta-blocker with this effect and evaluated their behaviour in cell lines. We identified molecular features that modulate this peculiar effect. In future, the understanding of this behaviour may contribute to an improved profile of beta-blockers leading to less side effects.