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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...
Regulation of Angiogenesis and Blood Supply01:24

Regulation of Angiogenesis and Blood Supply

Rapidly dividing tumors, embryos, and wounded tissues require more oxygen than usual, lowering the oxygen concentration in the blood. At low oxygen or hypoxic conditions, an oxygen-sensitive transcription factor called the hypoxia-inducible factor 1 or HIF1 is activated. HIF1 is a dimeric protein of alpha (ɑ) and beta (β) subunits.  Under optimal oxygen conditions, HIF1β is present in the nucleus while HIF1ɑ remains in the cytosol. HIF1ɑ is hydroxylated by prolyl hydroxylase and factor...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

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...
Hormonal Regulation of Blood Pressure01:17

Hormonal Regulation of Blood Pressure

Endocrinal or hormonal intervention in the cardiovascular system is predominantly exerted by the catecholamines - epinephrine and norepinephrine, as well as a slew of hormones that interact with renal function to modulate blood volume.
Epinephrine and Norepinephrine
The adrenal medulla releases epinephrine and norepinephrine, catecholamines that enhance and extend the sympathetic or "fight or flight" physiological response. These hormones escalate heart rate and the force of contraction while...
Vascular Spasm01:16

Vascular Spasm

The vascular phase, also known as vasospasm, is the initial stage of hemostasis, crucial for preventing excessive bleeding when a blood vessel is injured. After a vessel is cut, nerves in the damaged area trigger pain and other sensory impulses. Simultaneously, the smooth muscles in the vessel wall contract, resulting in a vascular spasm. This contraction reduces the vessel's diameter at the injury site, slowing or stopping blood loss through the vessel wall. Vascular spasms typically last for...
Hormonal Regulation01:33

Hormonal Regulation

The renin-aldosterone system is an endocrine system which guides the renal absorption of water and electrolytes, thus managing blood pressure and osmoregulation. Activation of the system begins in the kidneys with a small cluster of cells adjacent to the afferent and efferent blood vessels of the renal corpuscle. As the nephrons are filtering blood, juxtaglomerular cells monitor blood pressure. If they detect a decrease in pressure, they release the hormone renin into the bloodstream.

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Related Experiment Video

Updated: Jun 8, 2026

Precision Cut Lung Slices as an Efficient Tool for Ex vivo Pulmonary Vessel Structure and Contractility Studies
09:08

Precision Cut Lung Slices as an Efficient Tool for Ex vivo Pulmonary Vessel Structure and Contractility Studies

Published on: May 24, 2021

Endothelin.

Yoshifumi Kawanabe1, Surya M Nauli

  • 1Department of Neurosurgery, Otsu Municipal Hospital, Shiga, Japan. bwh5255725@yahoo.co.jp

Cellular and Molecular Life Sciences : CMLS
|September 18, 2010
PubMed
Summary

Endothelin-1, a potent vasoconstrictor, plays key roles in cardiovascular diseases and cancers. Research is rapidly advancing with selective endothelin receptor antagonists, offering new therapeutic avenues.

Area of Science:

  • Cardiovascular Physiology
  • Endocrinology
  • Oncology

Background:

  • Endothelin-1 (ET-1) is the most potent vasoconstrictor identified, originating from endothelial cells.
  • Two isoforms (ET-2, ET-3) and sarafotoxins have been identified, alongside endothelin-converting enzymes and receptors.
  • This review focuses on ET-1's clinical relevance, providing concise background information.

Purpose of the Study:

  • To review the basic science of endothelins, their converting enzymes, and receptors.
  • To describe the pathophysiological roles of ET-1 in major diseases.
  • To summarize pharmacological interventions and highlight recent research.

Main Methods:

  • Literature review of basic and clinical studies on endothelins.
  • Focus on endothelin-1's role in pulmonary arterial hypertension, heart failure, systemic hypertension, and ovarian cancer.

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  • Summary of pre-clinical and clinical data on endothelin receptor antagonists.

    • Main Results:

    • Endothelin-1 is implicated in the pathophysiology of cardiovascular diseases and certain malignancies.
    • Selective endothelin receptor antagonists show significant therapeutic potential.
    • Rapid advancements in the field are driven by new pharmacological agents.

    Conclusions:

    • Endothelin-1 is a critical mediator in various diseases, making it a therapeutic target.
    • Pharmacological targeting of endothelin receptors is a promising strategy.
    • The development of selective antagonists has accelerated research and therapeutic development in the endothelin field.