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Antihypertensive Drugs: Angiotensin II Receptor Blockers

Antihypertensive Drugs: Angiotensin II Receptor Blockers

In the renin-angiotensin-aldosterone system, a hormone called angiotensin II plays a crucial role. It binds to the AT1 receptors in vascular smooth muscles coupled with Gq proteins. The activation of these receptors activates an enzyme called phospholipase C, which releases two molecules: inositol trisphosphate and diacylglycerol. These molecules cause a chain reaction that leads to the phosphorylation of myosin light chains and promotes interaction between actin and myosin, leading to smooth...

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...

Antihypertensive Drugs: Direct Renin Inhibitors

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...

Transducer Mechanism: Enzyme-Linked Receptors

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...

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Related Experiment Video

Updated: May 29, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

[Angiotensin receptor vaccines].

Hiroyuki Sasamura¹, Tatsuhiko Azegami, Hiroshi Itoh

¹Department of Internal Medicine, Keio University.

Nihon Rinsho. Japanese Journal of Clinical Medicine

|September 20, 2011

Summary

Vaccines targeting the renin-angiotensin system (RAS) show promise in lowering blood pressure and preventing complications like organ damage. An angiotensin vaccine significantly reduced blood pressure in a recent clinical trial.

Area of Science:

Cardiovascular Research
Immunology
Pharmacology

Context:

Renin-angiotensin system (RAS) inhibitors prevent end-organ damage, hypertension, diabetes, and atrial fibrillation.
Vaccines against the RAS have been researched since the 1950s.

Purpose:

To evaluate the efficacy of an angiotensin vaccine in reducing blood pressure and preventing related complications.
To investigate the potential of targeting the angiotensin type 1 (AT1) receptor with vaccines.

Summary:

A phase IIa placebo-controlled study demonstrated that an angiotensin vaccine significantly decreases blood pressure in hypertensive patients.
Animal studies indicate vaccination against the AT1 receptor lowers blood pressure and ameliorates hypertensive end-organ damage.

More Related Videos

Live Cell Imaging and 3D Analysis of Angiotensin Receptor Type 1a Trafficking in Transfected Human Embryonic Kidney Cells Using Confocal Microscopy

Live Cell Imaging and 3D Analysis of Angiotensin Receptor Type 1a Trafficking in Transfected Human Embryonic Kidney Cells Using Confocal Microscopy

Published on: March 27, 2017

Isolation and Adoptive Transfer of High Salt Treated Antigen-presenting Dendritic Cells

Isolation and Adoptive Transfer of High Salt Treated Antigen-presenting Dendritic Cells

Published on: March 5, 2019

Related Experiment Videos

Last Updated: May 29, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

Live Cell Imaging and 3D Analysis of Angiotensin Receptor Type 1a Trafficking in Transfected Human Embryonic Kidney Cells Using Confocal Microscopy

Live Cell Imaging and 3D Analysis of Angiotensin Receptor Type 1a Trafficking in Transfected Human Embryonic Kidney Cells Using Confocal Microscopy

Published on: March 27, 2017

Isolation and Adoptive Transfer of High Salt Treated Antigen-presenting Dendritic Cells

Isolation and Adoptive Transfer of High Salt Treated Antigen-presenting Dendritic Cells

Published on: March 5, 2019

Impact:

Angiotensin receptor blockade via vaccination presents a novel therapeutic strategy for hypertension management.
This approach may prevent hypertension and its associated complications, offering a new avenue for cardiovascular disease prevention.