|endothelin receptor type A|
|Locus||Chr. 4 q31.2|
|endothelin receptor type B|
|Alt. symbols||HSCR2, HSCR|
|Locus||Chr. 13 q22|
There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium, which constricts the smooth muscles of the blood vessels, raising blood pressure, or relaxes the smooth muscles of the blood vessels, lowering blood pressure, among other functions.
- ETA is a subtype for vasoconstriction These receptors are found in the smooth muscle tissue of blood vessels, and binding of endothelin to ETA increases vasoconstriction (contraction of the blood vessel walls) and the retention of sodium, leading to increased blood pressure.
- ETB1 mediates vasodilation, When endothelin binds to ETB1 receptors, this leads to the release of nitric oxide (also called endothelium-derived relaxing factor), natriuresis and diuresis (the production and elimination of urine) and mechanisms that lower blood pressure.
- ETB2 mediates vasoconstriction
- ETC has yet no clearly defined function.
- ET receptor are also 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.
A similar strong vasoconstrictor action of endothelin-1 was demonstrated in a peripheral neuropathy model in rats.
Mutations in the EDNRB gene are associated with ABCD syndrome and some forms of Waardenburg syndrome.
- ↑ 1.0 1.1 1.2 1.3 1.4 Walter F. Boron, Emile L. Boulpaep, eds. (2009). Medical physiology a cellular and molecular approach (2nd ed.). Philadelphia, PA: Saunders/Elsevier. p. 480. ISBN 9781437720174.
- ↑ Davenport AP (2002). "International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature". Pharmacol. Rev. 54 (2): 219–26. CiteSeerX 10.1.1.546.8632. doi:10.1124/pr.54.2.219. PMID 12037137.
- ↑ Hynynen MM, Khalil RA; Khalil (January 2006). "The vascular endothelin system in hypertension--recent patents and discoveries". Recent Pat Cardiovasc Drug Discov. 1 (1): 95–108. doi:10.2174/157489006775244263. PMC 1351106. PMID 17200683.
- ↑ Barnes K, Turner AJ; Turner (August 1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and cellular studies". Neurochem. Res. 22 (8): 1033–40. doi:10.1023/A:1022435111928. PMID 9239759.
- ↑ Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF (July 1992). "Intraventricular endothelin-1 uncouples the blood flow: metabolism relationship in periventricular structures of the rat brain: involvement of L-type calcium channels". Neuropeptides. 22 (3): 155–65. doi:10.1016/0143-4179(92)90158-S. PMID 1331845.
- ↑ Zochodne DW, Ho LT, Gross PM (December 1992). "Acute endoneurial ischemia induced by epineurial endothelin in the rat sciatic nerve". Am. J. Physiol. 263 (6 Pt 2): H1806–10. doi:10.1152/ajpheart.1992.263.6.H1806. PMID 1481904.
- ↑ Verheij JB, Kunze J, Osinga J, van Essen AJ, Hofstra RM (2002). "ABCD syndrome is caused by a homozygous mutation in the EDNRB gene". Am. J. Med. Genet. 108 (3): 223–5. doi:10.1002/ajmg.10172. PMID 11891690.
- ↑ Read AP, Newton VE (1997). "Waardenburg syndrome". J. Med. Genet. 34 (8): 656–65. doi:10.1136/jmg.34.8.656. PMC 1051028. PMID 9279758.
- Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, Pollock DM, Webb DJ, Maguire JJ. (2016) 'Endothelin' Pharmacol. Rev. 68: 357-418. pmid =26956245 doi =10.1124/pr.115.011833
- "Endothelin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Endothelin+receptor at the US National Library of Medicine Medical Subject Headings (MeSH)
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