Počet záznamů: 1  

Epoxyeicosatrienoic acid analogue lowers blood pressure through vasodilation and sodium channel inhibition

  1. 1.
    0429211 - FGÚ 2015 RIV GB eng J - Článek v odborném periodiku
    Khan, M. A. H. - Pavlov, T. S. - Christain, S. V. - Neckář, Jan - Staruschenko, A. - Gauthier, K. M. - Capdevila, J. H. - Falck, J. R. - Campbell, W. B. - Imig, J. D.
    Epoxyeicosatrienoic acid analogue lowers blood pressure through vasodilation and sodium channel inhibition.
    Clinical science. Roč. 127, č. 7 (2014), s. 463-474. ISSN 0143-5221. E-ISSN 1470-8736
    Institucionální podpora: RVO:67985823
    Klíčová slova: angiotensin II * epithelial sodium channel (ENaC) * epoxyeicosatrienoic acid analogue * hypertension
    Kód oboru RIV: FA - Kardiovaskulární nemoci vč. kardiochirurgie
    Impakt faktor: 5.598, rok: 2014

    In the present study, multiple structural EET analogues were synthesized based on the EET pharmacophore and vasodilator structure-activity studies. Two EET analogues in which the COOH group at carbon 1 of the EET pharmacophore was replaced with either an aspartic acid (EET-A) or a heterocyclic surrogate (EET-X) lowered blood pressure in spontaneously hypertensive rats and in angiotensin II (AngII) hypertension. Additional experiments demonstrated that EET-A inhibits epithelial sodium channel (ENaC) activity in cultured cortical collecting duct cells and reduced renal expression of ENaC subunits in AngII hypertension. In conclusion, we have characterized EET-A as an orally active antihypertensive EET analogue that protects vascular endothelial function and has ENaC inhibitory activity in AngII hypertension
    Trvalý link: http://hdl.handle.net/11104/0234386

     
     
Počet záznamů: 1  

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