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19-Hydroxyeicosatetraenoic acid analogs: Antagonism of 20-hydroxyeicosatetraenoic acid-induced vascular sensitization and hypertension.

Abstract：

:19-Hydroxyeicosatetraenoic acid (19-HETE, 1), a metabolically and chemically labile cytochrome P450 eicosanoid, has diverse biological activities including antagonism of the vasoconstrictor 20-hydroxyeicosatetraenoic acid (20-HETE, 2). A SAR study was conducted to develop robust analogs of 1 with improved in vitro and in vivo efficacy. Analogs were screened in vitro for inhibition of 20-HETE-induced sensitization of rat renal preglomerular microvessels toward phenylephrine and demonstrated to normalize the blood pressure of male Cyp4a14(-/-) mice that display androgen-driven, 20-HETE-dependent hypertension.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Dakarapu R,Errabelli R,Manthati VL,Michael Adebesin A,Barma DK,Barma D,Garcia V,Zhang F,Laniado Schwartzman M,Falck JR

doi

10.1016/j.bmcl.2019.08.020

subject

Has Abstract

pub_date

2019-10-01 00:00:00

pages

126616

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30548-7

journal_volume

29

pub_type

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