Endothelin: Difference between revisions
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{{Short description|Peptides involved in vasoconstriction}} | |||
{{DISPLAYTITLE:Endothelin}} | |||
[[File:1EDN_human_endothelin1_02.png|Structure of human endothelin-1 | [[File:1EDN_human_endothelin1_02.png|thumb|right|Structure of human endothelin-1]] | ||
''' | '''Endothelins''' are a group of peptides with potent [[vasoconstrictor]] properties, playing a crucial role in the regulation of [[vascular tone]] and [[blood pressure]]. They are primarily produced by [[endothelial cells]] and have significant effects on various [[organ systems]]. | ||
== Structure == | ==Structure and Isoforms== | ||
Endothelins are small peptides consisting of 21 amino acids. | Endothelins are small [[peptides]] consisting of 21 [[amino acids]]. There are three isoforms of endothelin: [[endothelin-1]] (ET-1), [[endothelin-2]] (ET-2), and [[endothelin-3]] (ET-3). Each isoform is encoded by a separate gene and has distinct tissue distribution and physiological roles. | ||
== | ===Endothelin-1=== | ||
ET-1 is the most studied and is primarily involved in the regulation of [[vascular tone]]. It is produced by endothelial cells and acts in a paracrine manner to induce vasoconstriction. ET-1 is also involved in [[cell proliferation]], [[inflammation]], and [[fibrosis]]. | |||
=== Endothelin- | ===Endothelin-2 and Endothelin-3=== | ||
ET-2 and ET-3 have similar structures to ET-1 but differ in their tissue distribution and function. ET-2 is found in the [[kidneys]] and [[intestines]], while ET-3 is primarily located in the [[central nervous system]] and [[gastrointestinal tract]]. | |||
== | ==Receptors== | ||
Endothelins exert their effects through binding to specific [[G protein-coupled receptors]]: [[endothelin receptor type A]] (ETA) and [[endothelin receptor type B]] (ETB). ETA receptors are primarily located on [[vascular smooth muscle cells]] and mediate vasoconstriction. ETB receptors are found on endothelial cells and can mediate both vasodilation and vasoconstriction, depending on the context. | |||
== | ==Physiological Roles== | ||
Endothelins are involved in various physiological processes, including: | |||
* '''Regulation of Vascular Tone:''' Endothelins are key regulators of blood vessel constriction and dilation, influencing blood pressure and flow. | |||
* '''Cardiac Function:''' They play a role in [[cardiac contractility]] and [[heart rate]] regulation. | |||
* '''Renal Function:''' Endothelins affect [[glomerular filtration rate]] and [[sodium]] excretion, impacting [[fluid balance]]. | |||
* '''Neural Activity:''' In the [[central nervous system]], endothelins modulate [[neurotransmitter]] release and [[neuronal]] excitability. | |||
== Related | ==Pathophysiology== | ||
Dysregulation of endothelin production or receptor activity is implicated in several [[diseases]]: | |||
* '''Hypertension:''' Overproduction of ET-1 can lead to sustained vasoconstriction and elevated blood pressure. | |||
* '''Heart Failure:''' Endothelins contribute to [[cardiac remodeling]] and [[myocardial]] dysfunction. | |||
* '''Pulmonary Arterial Hypertension (PAH):''' Increased endothelin activity is a hallmark of PAH, leading to elevated pulmonary vascular resistance. | |||
* '''Renal Disease:''' Endothelins are involved in the progression of [[chronic kidney disease]] and [[glomerulonephritis]]. | |||
==Therapeutic Implications== | |||
Endothelin receptor antagonists, such as [[bosentan]] and [[ambrisentan]], are used in the treatment of conditions like pulmonary arterial hypertension. These drugs block the effects of endothelins, reducing vasoconstriction and improving blood flow. | |||
==Related Pages== | |||
* [[Vasoconstriction]] | * [[Vasoconstriction]] | ||
* [[ | * [[Endothelial cell]] | ||
* [[Pulmonary arterial hypertension]] | * [[Pulmonary arterial hypertension]] | ||
* [[G protein-coupled receptor]] | |||
* [[G | |||
[[Category:Peptides]] | [[Category:Peptides]] | ||
[[Category:Vasoconstrictors]] | |||
[[Category:Cardiovascular physiology]] | [[Category:Cardiovascular physiology]] | ||
Latest revision as of 17:17, 5 March 2025
Peptides involved in vasoconstriction
Endothelins are a group of peptides with potent vasoconstrictor properties, playing a crucial role in the regulation of vascular tone and blood pressure. They are primarily produced by endothelial cells and have significant effects on various organ systems.
Structure and Isoforms[edit]
Endothelins are small peptides consisting of 21 amino acids. There are three isoforms of endothelin: endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin-3 (ET-3). Each isoform is encoded by a separate gene and has distinct tissue distribution and physiological roles.
Endothelin-1[edit]
ET-1 is the most studied and is primarily involved in the regulation of vascular tone. It is produced by endothelial cells and acts in a paracrine manner to induce vasoconstriction. ET-1 is also involved in cell proliferation, inflammation, and fibrosis.
Endothelin-2 and Endothelin-3[edit]
ET-2 and ET-3 have similar structures to ET-1 but differ in their tissue distribution and function. ET-2 is found in the kidneys and intestines, while ET-3 is primarily located in the central nervous system and gastrointestinal tract.
Receptors[edit]
Endothelins exert their effects through binding to specific G protein-coupled receptors: endothelin receptor type A (ETA) and endothelin receptor type B (ETB). ETA receptors are primarily located on vascular smooth muscle cells and mediate vasoconstriction. ETB receptors are found on endothelial cells and can mediate both vasodilation and vasoconstriction, depending on the context.
Physiological Roles[edit]
Endothelins are involved in various physiological processes, including:
- Regulation of Vascular Tone: Endothelins are key regulators of blood vessel constriction and dilation, influencing blood pressure and flow.
- Cardiac Function: They play a role in cardiac contractility and heart rate regulation.
- Renal Function: Endothelins affect glomerular filtration rate and sodium excretion, impacting fluid balance.
- Neural Activity: In the central nervous system, endothelins modulate neurotransmitter release and neuronal excitability.
Pathophysiology[edit]
Dysregulation of endothelin production or receptor activity is implicated in several diseases:
- Hypertension: Overproduction of ET-1 can lead to sustained vasoconstriction and elevated blood pressure.
- Heart Failure: Endothelins contribute to cardiac remodeling and myocardial dysfunction.
- Pulmonary Arterial Hypertension (PAH): Increased endothelin activity is a hallmark of PAH, leading to elevated pulmonary vascular resistance.
- Renal Disease: Endothelins are involved in the progression of chronic kidney disease and glomerulonephritis.
Therapeutic Implications[edit]
Endothelin receptor antagonists, such as bosentan and ambrisentan, are used in the treatment of conditions like pulmonary arterial hypertension. These drugs block the effects of endothelins, reducing vasoconstriction and improving blood flow.
