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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

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...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Antihypertensive Drugs: Direct Renin Inhibitors01:25

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,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

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...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Antihypertensive Drugs: Angiotensin II Receptor Blockers01:30

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...

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Related Experiment Video

Updated: Jun 29, 2026

Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis
06:59

Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis

Published on: August 26, 2025

Ambrisentan.

Jamie D Croxtall1, Susan J Keam

  • 1Wolters Kluwer Health | Adis, Auckland, New Zealand. demail@adis.co.nz

Drugs
|October 9, 2008
PubMed
Summary
This summary is machine-generated.

Ambrisentan significantly improved exercise capacity and functional class in patients with pulmonary arterial hypertension (PAH). This oral ETA receptor antagonist demonstrated sustained benefits and favorable survival rates in clinical trials.

Related Experiment Videos

Last Updated: Jun 29, 2026

Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis
06:59

Catheter-based Endovascular Angioplasty for Fibrosing Mediastinitis-associated Pulmonary Vein Stenosis

Published on: August 26, 2025

Area of Science:

  • Cardiology
  • Pulmonology
  • Pharmacology

Background:

  • Elevated endothelin-1 (ET-1) is linked to pulmonary arterial hypertension (PAH) pathogenesis and prognosis.
  • Ambrisentan is a selective endothelin ETA receptor antagonist.

Purpose of the Study:

  • To evaluate the efficacy and safety of ambrisentan in patients with PAH.
  • To assess ambrisentan's impact on exercise capacity, clinical worsening, and functional status.

Main Methods:

  • Two Phase III, 12-week, placebo-controlled trials (ARIES-1 and ARIES-2) involving patients with WHO group I PAH.
  • Patients received ambrisentan (2.5-10 mg once daily) or placebo.
  • An extension trial (ARIES-E) assessed long-term effects.

Main Results:

  • Ambrisentan significantly increased 6-minute walk distance compared to placebo.
  • It delayed the incidence of clinical worsening and improved WHO functional class and Borg dyspnoea scores.
  • Benefits were maintained at 48 weeks, with one-year survival rates of 95-97%.

Conclusions:

  • Ambrisentan is an effective treatment for PAH, improving exercise capacity and functional status.
  • Long-term treatment with ambrisentan is generally well tolerated and associated with high survival rates.