AT1 Inhibitors

AT1 inhibitors, also known as angiotensin II receptor blockers (ARBs), are a class of compounds that selectively bind to the angiotensin II type 1 (AT1) receptor. Angiotensin II is a potent vasoactive peptide that plays a critical role in the renin-angiotensin system (RAS), which regulates blood pressure and fluid balance. The AT1 receptor is one of two main receptor subtypes for angiotensin II and is primarily responsible for the well-known actions of angiotensin II, including vasoconstriction, aldosterone secretion, modification of cardiac and vascular structure, and the reabsorption of sodium. By inhibiting this receptor, AT1 inhibitors interfere with the binding of angiotensin II to its receptor, thus blocking the receptors activation. This class of compounds exhibits a high affinity for the AT1 receptor subtype, as opposed to the angiotensin II type 2 (AT2) receptor, which has different and less well-understood functions.The chemical structure of AT1 inhibitors is characterized by a diversity of molecular frameworks, although many share common features that are essential for their activity. Typically, they possess a biphenyl moiety or an analogous non-biphenyl structure that allows for the proper spatial orientation necessary to interact with the AT1 receptor. Additionally, a carboxylic acid group or its bioisostere is commonly present, which is critical for binding to the receptor. The structural diversity among AT1 inhibitors allows for variations in their pharmacokinetic profiles and receptor binding dynamics.