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Endotelini su peptidi sa receptorskim i drugim efektima na mnoge tjelesne organe.[ 1] [ 2] [ 3] krvne sudove i podiže krvni pritisak . Endotelini se normalno održavaju u ravnoteži drugim mehanizmima, ali kada prekomjerno eksprimiraju , doprinose visokom krvnom pritisku (hipertenzija , srčanim i potencijalno drugim bolestima).[ 1] [ 4]
Endotelini su 21-aminokiselinaki vazokonstrikcijski peptidi proizvedeni prvenstveno u endotelu , koji imaju ključnu ulogu u vaskularnoj homeostazi . Endotelini su uključeni u vaskularne bolesti nekoliko organskih sistema, uključujući srce , pluća , bubrege i mozak .[ 5] [ 6] kliničkim istraživanjem , kako bi se definirala njihova uloga u nekoliko organskih sistema.[ 1] [ 7] [ 8] [ 9]
Poznate su tri izoforme (ET-1, -2, -3), sa različitim regionima ispoljavanja, i dva ključna tipa receptora , ETA i ETB .
Receptori za endotelin su različitoo ispoljeni u tijelu. Oni su prisutni u krvnim sudovima i ćelijama mozga, horoidnom pleksusu i perifernim nervima . Kada je ubrizgan direktno na mozak pacova u pikomolarnim količinama kao modelni organizam endotelin-1 uzrokuje snažnu metaboličku stimulaciju moždanog udara i epileptičke napade sa znatnim sniženjem dotoka krvi do pogođenih moždanih područja. Oba efekta su posredovana kalcijskim kanalima .[ 12]
^ a b c Davenport AP, Hyndman KA, Dhaun N, Southan C, Kohan DE, Pollock JS, et al. (april 2016). "Endothelin" . Pharmacological Reviews . 68 (2): 357–418. doi :10.1124/pr.115.011833 . PMC 4815360 PMID 26956245 . ^ Kawanabe Y, Nauli SM (januar 2011). "Endothelin" . Cellular and Molecular Life Sciences . 68 (2): 195–203. doi :10.1007/s00018-010-0518-0 . PMC 3141212 PMID 20848158 . ^ Kedzierski RM, Yanagisawa M (2001). "Endothelin system: the double-edged sword in health and disease" . Annual Review of Pharmacology and Toxicology . 41 : 851–76. doi :10.1146/annurev.pharmtox.41.1.851 . PMID 11264479 . ^ Maguire JJ, Davenport AP (decembar 2014). "Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12" . British Journal of Pharmacology . 171 (24): 5555–72. doi :10.1111/bph.12874 . PMC 4290702 PMID 25131455 . ^ Agapitov AV, Haynes WG (mart 2002). "Role of endothelin in cardiovascular disease". Journal of the Renin-Angiotensin-Aldosterone System . 3 (1): 1–15. doi :10.3317/jraas.2002.001 . PMID 11984741 . ^ Schinelli S (2006). "Pharmacology and physiopathology of the brain endothelin system: an overview". Current Medicinal Chemistry . 13 (6): 627–38. doi :10.2174/092986706776055652 . PMID 16529555 . ^ Kuang HY, Wu YH, Yi QJ, Tian J, Wu C, Shou WN, Lu TW (mart 2018). "The efficiency of endothelin receptor antagonist bosentan for pulmonary arterial hypertension associated with congenital heart disease: A systematic review and meta-analysis" . Medicine . 97 (10): e0075. doi :10.1097/MD.0000000000010075 . PMC 5882424 PMID 29517668 . ^ Iljazi A, Ayata C, Ashina M, Hougaard A (mart 2018). "The Role of Endothelin in the Pathophysiology of Migraine-a Systematic Review". Current Pain and Headache Reports . 22 (4): 27. doi :10.1007/s11916-018-0682-8 . PMID 29557064 . ^ Lu YP, Hasan AA, Zeng S, Hocher B (2017). "Plasma ET-1 Concentrations Are Elevated in Pregnant Women with Hypertension -Meta-Analysis of Clinical Studies" . Kidney & Blood Pressure Research . 42 (4): 654–663. doi :10.1159/000482004 PMID 29212079 . ^ Hynynen MM, Khalil RA (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 (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 (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 . CS1 održavanje: više imena: authors list (link )
Šablon:Peptidergici
