Endothelin

Endothelin 3
Identifiers
Symbol	EDN3
HUGO	3178
OMIM	131242
RefSeq	NM_000114
UniProt	P14138
Other data
Locus	Chr. 20 q13.2-q13.3

Endothelin 2
Identifiers
Symbol	EDN2
Entrez	1907
HUGO	3177
OMIM	131241
RefSeq	NM_001956
UniProt	P20800
Other data
Locus	Chr. 1 p34

Endothelin 1
Identifiers
Symbol	EDN1
Entrez	1906
HUGO	3176
OMIM	131240
RefSeq	NM_001955
UniProt	P05305
Other data
Locus	Chr. 6 p23-p24

Articles
WikiDoc Resources for Endothelin
Most recent articles on Endothelin Most cited articles on Endothelin Review articles on Endothelin Articles on Endothelin in N Eng J Med, Lancet, BMJ
Media
Powerpoint slides on Endothelin Images of Endothelin Photos of Endothelin Podcasts & MP3s on Endothelin Videos on Endothelin
Evidence Based Medicine
Cochrane Collaboration on Endothelin Bandolier on Endothelin TRIP on Endothelin
Clinical Trials
Ongoing Trials on Endothelin at Clinical Trials.gov Trial results on Endothelin Clinical Trials on Endothelin at Google
Guidelines / Policies / Govt
US National Guidelines Clearinghouse on Endothelin NICE Guidance on Endothelin NHS PRODIGY Guidance FDA on Endothelin CDC on Endothelin
Books
Books on Endothelin
News
Endothelin in the news Be alerted to news on Endothelin News trends on Endothelin
Commentary
Blogs on Endothelin
Definitions
Definitions of Endothelin
Patient Resources / Community
Patient resources on Endothelin Discussion groups on Endothelin Patient Handouts on Endothelin Directions to Hospitals Treating Endothelin Risk calculators and risk factors for Endothelin
Healthcare Provider Resources
Symptoms of Endothelin Causes & Risk Factors for Endothelin Diagnostic studies for Endothelin Treatment of Endothelin
Continuing Medical Education (CME)
CME Programs on Endothelin
International
Endothelin en Espanol Endothelin en Francais
Business
Endothelin in the Marketplace Patents on Endothelin
Experimental / Informatics
List of terms related to Endothelin

Overview

Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium that plays a key part in vascular homeostasis. Among the strongest vasoconstrictors known, endothelins are implicated in vascular diseases of several organ systems, including the heart, general circulation and brain^[1]^[2].

Isoforms

There are three isoforms with varying regions of expression and two key receptor types, ET_A and ET_B.

ET_A receptors are found in the smooth muscle tissue of blood vessels, and binding of endothelin to ET_A increases vasoconstriction (contraction of the blood vessel walls) and the retention of sodium. These lead to increased blood pressure.
ET_B is primarily located on the endothelial cells that line the interior of the blood vessels. When endothelin binds to ET_B receptors, this leads to increased natriuresis and diuresis (the production and elimination of urine) and the release of nitric oxide (also called "NO" or endothelium-derived relaxing factor), all mechanisms that lower the blood pressure.
Both types of ET receptor are found in the nervous system where they may mediate neurotransmission and vascular functions.

Brain and nerves

Widely distributed in the body, receptors for endothelin are present in blood vessels and cells of the brain, choroid plexus and peripheral nerves. When applied directly to the brain of rats in picomolar quantities as an experimental model of stroke, endothelin-1 caused severe metabolic stimulation and seizures with substantial decreases in blood flow to the same brain regions, both effects mediated by calcium channels^[3]. A similar strong vasoconstrictor action of endothelin-1 was demonstrated in a peripheral neuropathy model in rats^[4].

Balance

In a healthy individual, a delicate balance between vasoconstriction and vasodilation is maintained by endothelin, calcitonin and other vasoconstrictors on the one hand and nitric oxide, prostacyclin and other vasodilators on the other.

Overproduction of endothelin in the lungs may cause pulmonary hypertension, which can sometimes be treated by the use of an endothelin receptor antagonist, such as bosentan or sitaxsentan. The latter drug selectively blocks endothelin A receptors, decreasing the vasoconstrictive actions and allowing for increased beneficial effects of endothelin B stimulation, such as nitric oxide production. The precise effects of endothelin B receptor activation depends on the type of cells involved.

References

↑ Agapitov AV, Haynes WG. Role of endothelin in cardiovascular disease. J Renin Angiotensin Aldosterone Syst. 2002 Mar;3(1):1-15.[1]
↑ Schinelli S. Pharmacology and physiopathology of the brain endothelin system: an overview. Curr Med Chem. 2006;13(6):627-38. [2]
↑ Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF. Intraventricular endothelin-1 uncouples the blood flow: metabolism relationship in periventricular structures of the rat brain: involvement of L-type calcium channels. Neuropeptides. 1992 Jul;22(3):155-65. [3]
↑ Zochodne DW, Ho LT, Gross PM. Acute endoneurial ischemia induced by epineurial endothelin in the rat sciatic nerve. Am J Physiol. 1992 Dec;263(6 Pt 2):H1806-10.[4]

External links

Endothelin science (Actelion Pharmaceuticals)
Endothelins at the US National Library of Medicine Medical Subject Headings (MeSH)

Template:WH Template:WikiDoc Sources

[1] Agapitov AV, Haynes WG. Role of endothelin in cardiovascular disease. J Renin Angiotensin Aldosterone Syst. 2002 Mar;3(1):1-15.[1]

[2] Schinelli S. Pharmacology and physiopathology of the brain endothelin system: an overview. Curr Med Chem. 2006;13(6):627-38. [2]

[3] Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF. Intraventricular endothelin-1 uncouples the blood flow: metabolism relationship in periventricular structures of the rat brain: involvement of L-type calcium channels. Neuropeptides. 1992 Jul;22(3):155-65. [3]

[4] Zochodne DW, Ho LT, Gross PM. Acute endoneurial ischemia induced by epineurial endothelin in the rat sciatic nerve. Am J Physiol. 1992 Dec;263(6 Pt 2):H1806-10.[4]

[1]

[2]

[3]

[4]