Antagonists of angiotensin AT₁ receptors

Česká verze

Authors: Pavol Ježko; Milan Remko
Authors place of work: Univerzita Komenského v Bratislave, Farmaceutická fakulta, Katedra farmaceutickej chémie
Published in the journal: Čes. slov. Farm., 2011; 60, 171-181
Category: Přehledy a odborná sdělení

Summary

The medicinal agents which block AT₁ receptors are used for the treatment of hypertension, cardiac failure, and renal diseases. In clinical practice they have been available already for 15 years. All antagonists of AT₁ receptors were projected without any knowledge of the space (3D) structure of the AT₁ receptor. At present several strategies of projecting antihypertensive drugs are used, which are based on the influence on a number of receptors (e.g. the endothelial ones), not only angiotensin AT₁ receptors. With the use of rational methods of drug projecting based on the knowledge of the spatial structure of the active site of the AT₁ receptor, a development of new highly effective ligands for the therapy of cardiovascular diseases will be made possible. In the future, a development of drugs can be expected, which will block not only the angiotensin AT₁ receptors, but which will be able to influence also other endogenous ligands, e.g. endothelin and nitric oxide.

Key words:
RAAS – AT₁ receptors – antagonists of AT₁ receptors

Zdroje

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