Characterization of endothelin receptors in the human umbilical artery and vein

British Journal of Pharmacology
G BogoniD Regoli

Abstract

The aim of the present study was to characterize pharmacologically endothelin receptors that are present in human umbilical vessels. 2. Endothelin-1 (ET-1) and endothelin-2 (ET-2) are potent stimulants of both the human umbilical artery (pEC50 7.9 and 7.5) and vein (pEC50 8.1 and 8.0). Endothelin-3 (ET-3) is inactive on the artery but contracts the vein (pEC50 7.6). IRL1620 is inactive in both vessels. The order of potency of agonists is suggestive of a typical ET(A) receptor in the artery (ET-1 = ET-2 > > ET-3) and a mixture of ET(A) and ET(B) receptors in the vein (ET-1 = ET-2 > or = ET-3). 3. The selective ET(A) receptor antagonist, BQ123, competitively inhibits the effect of ET-1 in the human umbilical artery (pA2 6.9), while in the vein, only a mixture of BQ123 and BQ788 (a selective ET(B) antagonist) weakly displaces to the right of the cumulative concentration-response curve to ET-1. Contractions induced by ET-3 in the vein are inhibited by BQ788 (pA2 7.6), but not by BQ123. 4. Inhibition of Ca2+ channels by nifedipine (0.1 microM) is accompanied by a significant decrease of the maximal response to ET-1 by 40% in the artery and by 30% in the vein. The response of the vein to ET-3 is almost abolished by nifedipine. 5. The...Continue Reading

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Citations

Sep 24, 2002·Pharmacology & Therapeutics·P D'Orléans-JusteJ C Honoré
Jan 10, 1998·British Journal of Pharmacology·J J MaguireA P Davenport
Jan 5, 2011·Journal of Cellular and Molecular Medicine·Zoltan GalajdaArpad Tosaki
Jun 30, 2015·Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology·Riazudin MohammedEduardo Villamor
Mar 13, 2012·Life Sciences·Matthijs G CompeerJo G R De Mey
Nov 6, 2008·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Slobodan M JankovicSrdjan Stefanovic
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May 28, 2008·Fetal Diagnosis and Therapy·Eva MildenbergerHans T Versmold
Dec 18, 2001·Journal of Cardiovascular Pharmacology·Alan R ConantAlec W M Simpson
Jul 29, 2010·Clinical Science·Nathan R Tykocki, Stephanie W Watts
May 5, 2018·The Journal of Obstetrics and Gynaecology Research·Margarida LorigoElisa Cairrao
Aug 11, 2018·Pediatric Surgery International·Victor M Salinas-TorresLaura E Martínez-de-Villarreal

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