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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

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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...
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Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

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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...
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Antihypertensive Drugs: Angiotensin II Receptor Blockers01:30

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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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Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...
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Antihypertensive Drugs: Direct Renin Inhibitors01:25

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

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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...
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Current Knowledge About Aprocitentan in Hypertension.

Emilie Mathilde Bank-Mikkelsen1, Daniela Grimm1,2, Markus Wehland2

  • 1Department of Biomedicine, Aarhus University, 8000 Aarhus, Denmark.

International Journal of Molecular Sciences
|December 11, 2025
PubMed
Summary
This summary is machine-generated.

Aprocitentan (ACT) effectively lowers high blood pressure (hypertension) within 14 days. This dual endothelin receptor antagonist shows promise for managing resistant hypertension with no severe side effects.

Keywords:
aprocitentandual endothelin receptor antagonisthypertension

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Area of Science:

  • Pharmacology
  • Cardiovascular Medicine
  • Clinical Therapeutics

Background:

  • Hypertension (HT) is a leading global health issue, increasing cardiovascular disease (CVD) risk.
  • HT is a modifiable risk factor, necessitating novel therapeutic strategies.
  • Rising life expectancy and obesity rates are exacerbating the global hypertension burden.

Purpose of the Study:

  • To review current knowledge on aprocitentan (ACT) for hypertension management.
  • To explore ACT's pharmacological mechanisms and therapeutic potential.
  • To assess ACT's role in addressing resistant hypertension.

Main Methods:

  • Conducted a literature search on PubMed and ClinicalTrials.gov.
  • Utilized search terms including "hypertension", "aprocitentan", "high blood pressure", and "cardiovascular disease".
  • Reviewed human and animal studies on ACT's efficacy and safety.

Main Results:

  • ACT demonstrated significant blood pressure reduction within 14 days in human and animal studies.
  • The optimal effective dose identified was 25 mg, with no severe adverse effects reported.
  • ACT showed compatibility with other antihypertensive agents, sometimes yielding synergistic effects.

Conclusions:

  • Aprocitentan (ACT) is a promising dual endothelin receptor antagonist for hypertension.
  • ACT may play a key role in managing resistant hypertension due to its unique mechanism of action.
  • Its compatibility with existing therapies suggests potential for combination use in complex cases.