NYMC Faculty Publications

Title

19-Hydroxyeicosatetraenoic Acid Analogs: Antagonism of 20-Hydroxyeicosatetraenoic Acid-Induced Vascular Sensitization and Hypertension

First Page

126616

Document Type

Article

Publication Date

October 2019

Department

Pharmacology

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.

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